Roberto Pellicciari

Roberto Pellicciari's AcademicInfluence.com Rankings

Roberto Pellicciari

Chemistry

#4786

World Rank

#5877

Historical Rank

Organic Chemistry

#795

World Rank

#894

Historical Rank

chemistry Degrees

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Chemistry

Roberto Pellicciari's Degrees

Bachelors Chemistry University of Bologna
PhD Chemical Biology University of California, San Francisco

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Roberto Pellicciari's Published Works

Number of citations in a given year to any of this author's works

Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author

Published Works

TGR5-mediated bile acid sensing controls glucose homeostasis. (2009) (1414)
Targeting bile-acid signalling for metabolic diseases (2008) (1082)
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. (2002) (656)
Manipulation of Brain Kynurenines: Glial Targets, Neuronal Effects, and Clinical Opportunities (2002) (545)
Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors (2012) (441)
TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading. (2011) (440)
The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis. (2004) (411)
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. (2008) (255)
Structural basis for bile acid binding and activation of the nuclear receptor FXR. (2003) (252)
De novo NAD+ synthesis enhances mitochondrial function and improves health (2018) (244)
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. (2009) (209)
Protective Effects of 6-Ethyl Chenodeoxycholic Acid, a Farnesoid X Receptor Ligand, in Estrogen-Induced Cholestasis (2005) (186)
Pharmacological characterization of 1-aminoindan-1,5-dicarboxylic acid, a potent mGluR1 antagonist. (1997) (178)
A Farnesoid X Receptor-Small Heterodimer Partner Regulatory Cascade Modulates Tissue Metalloproteinase Inhibitor-1 and Matrix Metalloprotease Expression in Hepatic Stellate Cells and Promotes Resolution of Liver Fibrosis (2005) (166)
The Farnesoid X Receptor Promotes Adipocyte Differentiation and Regulates Adipose Cell Function in Vivo (2006) (164)
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid. (2004) (162)
1-Aminoindan-1,5-dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors. (1995) (159)
Inhibitors of kynurenine hydroxylase and kynureninase increase cerebral formation of kynurenate and have sedative and anticonvulsant activities (1994) (158)
Cross-Talk between Farnesoid-X-Receptor (FXR) and Peroxisome Proliferator-Activated Receptor γ Contributes to the Antifibrotic Activity of FXR Ligands in Rodent Models of Liver Cirrhosis (2005) (155)
Protection with metabotropic glutamate 1 receptor antagonists in models of ischemic neuronal death: time-course and mechanisms (1999) (146)
TGR5 reduces macrophage migration through mTOR-induced C/EBPβ differential translation. (2014) (143)
Poly(ADP-ribose) polymerase inhibitors attenuate necrotic but not apoptotic neuronal death in experimental models of cerebral ischemia (2001) (141)
On the relationship between the two branches of the kynurenine pathway in the rat brain in vivo (2009) (139)
Fluctuations in Endogenous Kynurenic Acid Control Hippocampal Glutamate and Memory (2011) (138)
The Astrocyte-Derived α7 Nicotinic Receptor Antagonist Kynurenic Acid Controls Extracellular Glutamate Levels in the Prefrontal Cortex (2009) (134)
Modulation of the kynurenine pathway in search for new neuroprotective agents. Synthesis and preliminary evaluation of (m-nitrobenzoyl)alanine, a potent inhibitor of kynurenine-3-hydroxylase. (1994) (127)
Endogenous kynurenate controls the vulnerability of striatal neurons to quinolinate: Implications for Huntington's disease (2006) (118)
(S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist. (1996) (116)
Astrocyte‐derived kynurenic acid modulates basal and evoked cortical acetylcholine release (2009) (114)
Highlights at the gate of tryptophan catabolism: a review on the mechanisms of activation and regulation of indoleamine 2,3-dioxygenase (IDO), a novel target in cancer disease (2009) (113)
Modulation of Quinolinic and Kynurenic Acid Content in the Rat Brain: Effects of Endotoxins and Nicotinylalanine (1991) (109)
Comparison of the Neurochemical and Behavioral Effects Resulting from the Inhibition of Kynurenine Hydroxylase and/or Kynureninase (1995) (106)
Farnesoid X receptor: from structure to potential clinical applications. (2005) (101)
Role of FXR in regulating bile acid homeostasis and relevance for human diseases. (2005) (97)
C60 carboxyfullerene exerts a protective activity against oxidative stress-induced apoptosis in human peripheral blood mononuclear cells. (2000) (94)
Bile Acids Signal via TGR5 to Activate Intestinal Stem Cells and Epithelial Regeneration. (2020) (94)
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5. (2007) (92)
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis. (2001) (91)
Cortical kynurenic acid bi-directionally modulates prefrontal glutamate levels as assessed by microdialysis and rapid electrochemistry (2010) (89)
Specific inhibition of kynurenate synthesis enhances extracellular dopamine levels in the rodent striatum (2009) (88)
Nicotinylalanine Increases the Formation of Kynurenic Acid in the Brain and Antagonizes Convulsions (1992) (87)
Poly(ADP-ribose) Catabolism Triggers AMP-dependent Mitochondrial Energy Failure* (2009) (86)
C3‐Fullero‐tris‐Methanodicarboxylic Acid Protects Cerebellar Granule Cells from Apoptosis (2000) (86)
Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2'-carboxy-3'-phenylcyclopropyl)glycine. Focus on (2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a novel and selective group II metabotropic glutamate receptors antagonist. (1996) (80)
Type 2 Metabotropic Glutamate (mGlu) Receptors Tonically Inhibit Transmitter Release in Rat Caudate Nucleus: In Vivo Studies with (2S,1′S,2′S,3′R)‐2‐(2′‐carboxy‐3′‐phenylcyclopropyl)glycine, a New Potent and Selective Antagonist (1997) (80)
Presynaptic mGlu1 type receptors potentiate transmitter output in the rat cortex. (1998) (79)
Carboxyfullerenes protect human keratinocytes from ultraviolet-B-induced apoptosis. (2000) (78)
The Methyl Transferase PRMT1 Functions as Co-Activator of Farnesoid X Receptor (FXR)/9-cis Retinoid X Receptor and Regulates Transcription of FXR Responsive Genes (2005) (78)
Modulators of the Kynurenine Pathway of Tryptophan Metabolism: Synthesis and Preliminary Biological Evaluation of (S)‐4‐(Ethylsulfonyl)benzoylalanine, a Potent and Selective Kynurenine Aminotransferase II (KAT II) Inhibitor (2006) (74)
Novel Isoquinolinone-Derived Inhibitors of Poly(ADP-ribose) Polymerase-1: Pharmacological Characterization and Neuroprotective Effects in an in Vitro Model of Cerebral Ischemia (2003) (73)
Metabotropic G-protein-coupled glutamate receptors as therapeutic targets. (1999) (73)
The Reaction of α-Diazo-β-hydroxy Esters with Boron Trifluoride Etherate: Generation and Rearrangement of Destabilized Vinyl Cations. A Detailed Experimental and Theoretical Study (1996) (73)
Development of 1,2,4-Oxadiazoles as Potent and Selective Inhibitors of the Human Deacetylase Sirtuin 2: Structure-Activity Relationship, X-ray Crystal Structure, and Anticancer Activity. (2017) (72)
Progress and challenges of selective Farnesoid X Receptor modulation. (2018) (72)
Rat brain guanosine binding site. Biological studies and pseudo-receptor construction. (2003) (64)
Cyclopentanone synthesis by intramolecular carbon-hydrogen insertion of diazo ketones. A diterpene-to-steroid skeleton conversion (1982) (62)
Reactions of ethyl diazoacetate with thianaphthene, indoles, and benzofuran (1977) (62)
On the Way to Selective PARP‐2 Inhibitors. Design, Synthesis, and Preliminary Evaluation of a Series of Isoquinolinone Derivatives (2008) (60)
Metabotropic glutamate 1 (mGlu1) receptor antagonists enhance GABAergic neurotransmission: a mechanism for the attenuation of post-ischemic injury and epileptiform activity? (2002) (58)
Carboxyfullerenes localize within mitochondria and prevent the UVB‐induced intrinsic apoptotic pathway (2007) (56)
The novel and systemically active metabotropic glutamate 1 (mGlu1) receptor antagonist 3-MATIDA reduces post-ischemic neuronal death (2002) (54)
QSAR and molecular modeling studies of baclofen analogues as GABA(B) agonists. Insights into the role of the aromatic moiety in GABA(B) binding and activation. (2001) (53)
The structure of fusicoccin A (1968) (50)
Building a sulfonamide library by eco-friendly flow synthesis. (2013) (50)
Semisynthetic Bile Acid FXR and TGR5 Agonists: Physicochemical Properties, Pharmacokinetics, and Metabolism in the Rat (2014) (49)
Docking studies on PARP-1 inhibitors: insights into the role of a binding pocket water molecule. (2005) (48)
Long‐lasting neuroprotection and neurological improvement in stroke models with new, potent and brain permeable inhibitors of poly(ADP‐ribose) polymerase (2012) (48)
Homology modeling of metabotropic glutamate receptors. (mGluRs) structural motifs affecting binding modes and pharmacological profile of mGluR1 agonists and competitive antagonists. (1996) (47)
Synthesis and biological evaluation of 2-(3'-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist. (2001) (47)
Patented TGR5 modulators: a review (2006 – present) (2012) (46)
(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine, a potent and selective antagonist of type 2 metabotropic glutamate receptors. (1996) (46)
C3‐Fullero‐tris‐methanodicarboxylic acid protects epithelial cells from radiation‐induced anoikia by influencing cell adhesion ability (1999) (45)
Novel Polymorphisms of Nuclear Receptor SHP Associated with Functional and Structural Changes (2010) (45)
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives. (2006) (44)
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders. (2016) (42)
β-Keto esters from the rhodium(II) acetate catalysed conversion of α-diazo-β-hydroxy esters (1979) (42)
Synthesis and biological evaluation of cyclopropyl analogues of 2-amino-5-phosphonopentanoic acid. (2010) (40)
Selective PARP‐2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post‐ischaemic brain damage (2009) (40)
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine. (2011) (39)
Thiokynurenates: a new group of antagonists of the glycine modulatory site of the NMDA receptor. (1991) (38)
Beyond bile acids: targeting Farnesoid X Receptor (FXR) with natural and synthetic ligands. (2014) (38)
Continuous Flow Synthesis of Thieno[2,3-c]isoquinolin-5(4H)-one Scaffold: A Valuable Source of PARP-1 Inhibitors (2014) (38)
D-3,4-'cyclopropylglutamate' isomers as NMDA receptor ligands: synthesis and enantioselective activity (1990) (37)
Conservation of the ligand recognition site of metabotropic glutamate receptors during evolution (2000) (37)
Central anorexigenic actions of bile acids are mediated by TGR5 (2021) (36)
Molecular docking and spatial coarse graining simulations as tools to investigate substrate recognition, enhancer binding and conformational transitions in indoleamine-2,3-dioxygenase (IDO). (2007) (36)
Rhodium-catalysed redox isomerization of hydroxy alkynes to trans keto and hydroxy vinyl esters. A short and stereoselective synthesis of dipeptide isosters (1995) (36)
Probing the Binding Site of Bile Acids in TGR5. (2013) (36)
Exploring the other side of biologically relevant chemical space: insights into carboxylic, sulfonic and phosphonic acid bioisosteric relationships. (2007) (35)
From polypharmacology to target specificity: the case of PARP inhibitors. (2013) (35)
Adamantyl-substituted retinoid-derived molecules that interact with the orphan nuclear receptor small heterodimer partner: effects of replacing the 1-adamantyl or hydroxyl group on inhibition of cancer cell growth, induction of cancer cell apoptosis, and inhibition of SRC homology 2 domain-containin (2008) (34)
Targeting the MDM2/MDM4 interaction interface as a promising approach for p53 reactivation therapy. (2015) (34)
Biochemical and electrophysiological studies on (S)-(+)-2-(3′-carboxybicyclo[1.1.1]pentyl)-glycine (CBPG), a novel mGlu5 receptor agonist endowed with mGlu1 receptor antagonist activity (1999) (34)
S-trityl-(R)-cysteine, a powerful chiral selector for the analytical and preparative ligand-exchange chromatography of amino acids. (2008) (34)
Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists. (2012) (33)
Molecular dynamics simulation of the ligand binding domain of farnesoid X receptor. Insights into helix-12 stability and coactivator peptide stabilization in response to agonist binding. (2005) (32)
Dynamic ligand-exchange chiral stationary phase from S-benzyl-(R)-cysteine. (2006) (32)
Synthesis and preliminary evaluation of (S)-2-(4'-carboxycubyl)glycine, a new selective mGluR1 antagonist. (1998) (32)
Perinatal kynurenine 3‐hydroxylase inhibition in rodents: Pathophysiological implications (2007) (31)
Ursodeoxycholic acid attenuates colonic epithelial secretory function (2013) (31)
The depolarization-induced outflow of d-[3H]aspartate from rat brain slices is modulated by metabotropic glutamate receptors (1994) (30)
The effect of the copper(II) salt anion in the Chiral Ligand-Exchange Chromatography of amino acids. (2009) (30)
Targeting the Conformational Transitions of MDM2 and MDMX: Insights into Dissimilarities and Similarities of p53 Recognition (2008) (30)
Modulation of the kynurine pathway of tryptophan metabolism in search for neuroprotective agents. Focus on kynurenine-3-hydroxylase. (2003) (30)
Relationship between structure and intestinal absorption of bile acids with a steroid or side-chain modification (1996) (30)
Bile acid derivatives as ligands of the farnesoid x receptor: molecular determinants for bile acid binding and receptor modulation. (2014) (30)
Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors. (2014) (29)
Puzzling over MDM4-p53 network. (2010) (29)
Sequence Variants in Kynurenine Aminotransferase II (KAT II) Orthologs Determine Different Potencies of the Inhibitor S‐ESBA (2008) (28)
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. (2005) (28)
Human kynurenine aminotransferase II – reactivity with substrates and inhibitors (2011) (28)
Pharmacophore model for bile acids recognition by the FPR receptor (2006) (28)
Poly(ADP-ribose) polymerase inhibition with HYDAMTIQ reduces allergen-induced asthma-like reaction, bronchial hyper-reactivity and airway remodelling (2014) (27)
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. (2012) (26)
Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III. (2000) (26)
Preparative resolution of 1-aminoindan-1,5-dicarboxylic acid (AIDA) by chiral ligand-exchange chromatography. (2004) (26)
α-Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) Inhibitors as Novel Modulators of De Novo Nicotinamide Adenine Dinucleotide (NAD+) Biosynthesis. (2018) (26)
The glucocorticoid mometasone furoate is a novel FXR ligand that decreases inflammatory but not metabolic gene expression (2015) (25)
Bile acids with a cyclopropyl-containing side chain. IV. Physicochemical and biological properties of the four diastereoisomers of 3 alpha,7 beta-dihydroxy-22,23-methylene-5 beta-cholan-24-oic acid. (1987) (25)
7α-OH epimerisation of bile acids via oxido-reduction with Xanthomonas maltophilia (2002) (25)
Antagonist pharmacology of metabotropic glutamate receptors coupled to phospholipase D activation in adult rat hippocampus: focus on (2R,1'S,2'R,3'S)-2-(2'-carboxy-3'-phenylcyclopropyl)glycine versus 3, 5-dihydroxyphenylglycine. (1999) (25)
Rad51/BRCA2 disruptors inhibit homologous recombination and synergize with olaparib in pancreatic cancer cells. (2019) (25)
Ring expansion of thiochroman-4-one and isothiochroman-4-one with ethyl diazo(lithio)acetate to tetrahydrobenzothiepin beta-oxoesters. (1977) (25)
Synthesis and biological evaluation of (2S)- and (2R)-2-(3'-phosphonobicyclo[1.1.1]pentyl)glycines as novel group III selective metabotropic glutamate receptor ligands. (2006) (25)
Proteins: Structure, Function, and Bioinformatics (2009) (25)
Correlation between CMC and chromatographic index: simple and effective evaluation of the hydrophobic/hydrophilic balance of bile acids (2007) (25)
Concepts and Molecular Aspects in the Polypharmacology of PARP‐1 Inhibitors (2016) (25)
Exploring the synthetic versatility of the Lewis acid induced decomposition reaction of α-diazo-β-hydroxy esters. The case of ethyl diazo(3-hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)acetate. (2011) (25)
L-Vinylglycine from L-Homoserine. (1988) (24)
Cysteine-based chiral selectors for the ligand-exchange separation of amino acids. (2008) (24)
Molecular Field Analysis and 3D-Quantitative Structure-Activity Relationship Study (MFA 3D-QSAR) Unveil Novel Features of Bile Acid Recognition at TGR5 (2008) (24)
Synthesis and Preliminary Biological Evaluation of 2′‐Substituted 2‐(3′‐Carboxybicyclo[1.1.1]pentyl)glycine Derivatives as Group I Selective Metabotropic Glutamate Receptor Ligands (2006) (24)
Quantitative relationship between bile acid structure and biliary lipid secretion in rats. (1988) (24)
Spiro[2.2]pentane as a dissymmetric scaffold for conformationally constrained analogues of glutamic acid: focus on racemic 1-aminospiro[2.2]pentyl-1,4-dicarboxylic acids. (2002) (23)
Pharmacological inhibition of poly(ADP-ribose) polymerase (PARP) activity in PARP-1 silenced tumour cells increases chemosensitivity to temozolomide and to a N3-adenine selective methylating agent. (2010) (23)
Unveiling hidden features of orphan nuclear receptors: the case of the small heterodimer partner (SHP). (2006) (23)
Pharmacophore models of group I and group II metabotropic glutamate receptor agonists. Analysis of conformational, steric, and topological parameters affecting potency and selectivity. (1999) (23)
Enantioselective Synthesis of Naturally Occurring trans-4-Hydroxy-S-pipecolic Acid-4-sulfate, a New Potent and Selective NMDA Receptor Agonist (1992) (23)
Synthetic Lethality in Pancreatic Cancer: Discovery of a New RAD51-BRCA2 Small Molecule Disruptor That Inhibits Homologous Recombination and Synergizes with Olaparib (2020) (23)
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity. (1999) (23)
(2R,1'S,2'R,3'S)-2-(2'-Carboxy-3'-phenylcyclopropyl)glycine (PCCG-13), the first potent and selective competitive antagonist of phospholipase D-coupled metabotropic glutamate receptors: asymmetric synthesis and preliminary biological properties. (1999) (22)
23‐Methyl‐3α, 7β‐dihydroxy‐5β‐cholan‐24‐oic acid: Dose‐response study of biliary secretion in rat (1988) (22)
New one-pot synthesis of pyrazole-5-carboxylates by 1,3-dipole cycloadditions of ethyl diazoacetate with α-methylene carbonyl compounds (2009) (22)
Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR). (2003) (22)
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor (2019) (21)
Reduction of α-diazo-β-hydroxy esters to β-hydroxy esters: application in one of two convergent syntheses of a (22S)-22-hydroxy bile acid from fish bile and its (22R)-epimer (1985) (21)
Synthetic Lethality Triggered by Combining Olaparib with BRCA2-Rad51 Disruptors. (2017) (21)
O-Benzyl-(S)-Serine, a New Chiral Selector for Ligand-Exchange Chromatography of Amino Acids (2005) (21)
Towards new neuroprotective agents: design and synthesis of 4H-thieno[2,3-c] isoquinolin-5-one derivatives as potent PARP-1 inhibitors. (2003) (21)
Design, synthesis and preliminary evaluation of novel 3'-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors. (2001) (20)
Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists. (2018) (20)
Novel stereoselective synthesis and chromatographic evaluation of E-guggulsterone (2012) (19)
Dirhodium(II) Tetraacetate-Mediated Decomposition of Ethyldiazoacetate and Ethyldiazomalonate in the Presence of Fullerene. A New Procedure for the Selective Synthesis of [6-6]-Closed Methanofullerenes (1997) (19)
Physicochemical and biological properties of natural and synthetic C-22 and C-23 hydroxylated bile acids. (1990) (19)
PARP-1 and its inhibitors: molecular modeling studies (2003) (19)
Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands. (2009) (19)
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues. (2006) (19)
Synthesis and activity of enantiopure (S) (m-nitrobenzoyl) alanine, potent kynurenine-3-hydroxylase inhibitor (1995) (19)
Bile acids with a cyclopropyl-containing side chain. 1. Preparation and properties of 3 alpha, 7 beta-dihydroxy-22,23-methylene-5 beta-cholan-24-oic acid. (1984) (18)
Continuous flow synthesis and scale-up of glycine- and taurine-conjugated bile salts. (2012) (18)
BF(3).Et(2)O-induced decomposition of ethyl 2-diazo-3-hydroxy-3,3-diarylpropanoates in acetonitrile: a novel approach to 2,3-diaryl beta-enamino ester derivatives. (2009) (18)
Bile acids with cyclopropane-containing side chain. 2. Synthesis and properties of 3 alpha,7 beta-dihydroxy-22,23-methylene-5 beta-cholan-24-oic acid (2-sulfoethyl)amide. (1985) (18)
Brush-border-enzyme-mediated intestine-specific drug delivery. Amino acid prodrugs of 5-aminosalicylic acid. (1993) (17)
A new synthesis of carboxyterfenadine (fexofenadine) and its bioisosteric tetrazole analogs. (1999) (17)
(S)‐(–)‐α,α‐Di(2‐naphthyl)‐2‐pyrrolidinemethanol, a useful tool to study the recognition mechanism in chiral ligand‐exchange chromatography (2007) (17)
Computational studies for the elucidation of the enantiomer elution order of amino acids in chiral ligand-exchange chromatography. (2010) (17)
Farnesoid X Receptor: From Structure to Potential Clinical Applications (2005) (17)
Evaluation of the enantiomeric selectivity in the chiral ligand-exchange chromatography of amino acids by a computational model. (2004) (17)
Derived chromatographic indices as effective tools to study the self-aggregation process of bile acids. (2009) (17)
Indium triflate catalyzed reaction of diisopropyl diazomethylphosphonate with imines as a new approach to cis- and trans-aziridine-2-phosphonates (2007) (17)
Bile acids with a cyclopropyl-containing side chain. 3. Separation, identification, and properties of all four stereoisomers of 3 alpha,7 beta-dihydroxy-22,23-methylene-5 beta-cholan-24-oic acid. (1988) (16)
A new synthesis of -damascone (1980) (16)
Thermal and Catalytic Reactions of Diazoacetylmetallocenes with [60]Fullerene (2003) (16)
Expanding the horizon of chemotherapeutic targets: From MDM2 to MDMX (MDM4) (2011) (16)
QSAR study of anticonvulsant negative allosteric modulators of the AMPA receptor. (2004) (16)
Conformationally constrained amino acids: enantiodivergent synthesis of all four stereoisomers of 2-(tetrahydrofuran-2-yl)glycine (2005) (15)
Scaffold hopping approach on the route to selective tankyrase inhibitors. (2014) (15)
Asymmetric synthesis of the four diastereoisomers of a novel non-steroidal farnesoid X receptor (FXR) agonist: role of the chirality on the biological activity. (2013) (15)
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines. (2007) (15)
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs. (2007) (15)
Homology model of the multidrug transporter LmrA from Lactococcus lactis. (2004) (15)
Tandem mass spectrometric determination of atypical 3β-hydroxy-Δ5-bile acids in patients with 3β-hydroxy-Δ5-C27-steroid oxidoreductase deficiency: application to diagnosis and monitoring of bile acid therapeutic response. (2015) (15)
Exploring the effect of PARP-1 flexibility in docking studies. (2013) (14)
Discovery and characterization of novel potent PARP-1 inhibitors endowed with neuroprotective properties: From TIQ-A to HYDAMTIQ (2011) (14)
Sulfate esters of hydroxy amino acids as stereospecific glutamate receptor agonists. (1994) (14)
Modulation of glutamate receptor pathways in the search for new neuroprotective agents. (1998) (14)
Targeting the conformational transitions of MDM2 and MDMX: Insights into key residues affecting p53 recognition (2009) (14)
An improved two-step route for the preparation of β-diketones from aldehydes and its application to the synthesis of β-damascone (1982) (14)
Preparation of 1‐(Aroylalkyl)‐1H‐imidazole and ‐Benzimidazole Derivatives of Pharmaceutical Interest. A New Synthetic Procedure (1984) (13)
Conformationally constrained tryptophan analogs. Synthesis of (±)-(Z)- and (±)-(E)-2-amino-2,3-methano-3-(indol-3-yl)-propanoic acids (1996) (13)
New 6-substituted bile acids: physico-chemical and biological properties of 6 alpha-methyl ursodeoxycholic acid and 6 alpha-methyl-7-epicholic acid. (1994) (13)
Indoleamine 2,3-dioxygenase 1 activation in mature cDC1 promotes tolerogenic education of inflammatory cDC2 via metabolic communication (2022) (13)
Chiral ligand-exchange separation and resolution of extremely rigid glutamate analogs: 1-aminospiro[2.2]pentyl-1,4-dicarboxylic acids (2010) (13)
Metabolism, pharmacokinetics, and activity of a new 6-fluoro analogue of ursodeoxycholic acid in rats and hamsters. (1995) (13)
Potential therapeutic applications of farnesoid X receptor (FXR) modulators (2006) (13)
Synthesis of a novel, conformationally restricted analog of tryptophan (1993) (13)
Molecular Interaction Fields and 3D-QSAR Studies of p53-MDM2 Inhibitors Suggest Additional Features of Ligand-Target Interaction (2010) (13)
Divergent and stereoselective synthesis of dafachronic acids (2011) (13)
Glucuronidation of bile acids under flow conditions: design of experiments and Koenigs-Knorr reaction optimization. (2014) (13)
The role of electrostatic interaction in the molecular recognition of selective agonists to metabotropic glutamate receptors (2003) (12)
Reactions of Alkoxycarbonylcarbenoids with Imidazole; An Improved Preparation of Ethyl Imidazole-1-ylacetate and the First Synthesis of Diethyl Imidazole-1-ylmalonate (1981) (12)
Stereospecific synthesis of the enantiomers of nicotinylalanine, a neuroprotecting agent (1992) (12)
Structure-activity relationship studies on natural and synthetic bile acid analogs (1989) (12)
The reaction of α-diazo-β-hydroxy esters with boron trifluoride (1993) (12)
Insights into Phenylalanine Derivatives Recognition of VLA-4 Integrin: From a Pharmacophoric Study to 3D-QSAR and Molecular Docking Analyses (2004) (12)
A highly selective agonist for the metabotropic glutamate receptor mGluR2 (2011) (11)
Synthesis of atypical bile acids for use as investigative tools for the genetic defect of 3β-hydroxy-Δ5-C27-steroid oxidoreductase deficiency (2014) (11)
Fast chromatographic determination of the bile salt critical micellar concentration (2011) (11)
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MDM2/MDMX inhibitor peptide: WO2008106507 (2009) (11)
Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification. (2018) (11)
Investigating the allosteric reverse signalling of PARP inhibitors with microsecond molecular dynamic simulations and fluorescence anisotropy. (2014) (11)
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Amino acid derivatives of 5-ASA as novel prodrugs for intestinal drug delivery (1994) (10)
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Metabotropic glutamate receptors: structure and new subtype-selective ligands. (2001) (10)
Stereoselective synthesis and preliminary evaluation of (+)- and (-)-3-methyl-5-carboxy-thien-2-yl-glycine (3-MATIDA): identification of (+)-3-MATIDA as a novel mGluR1 competitive antagonist. (2004) (10)
Poly(ADP‐Ribose)‐Polymerase‐Catalyzed Hydrolysis of NAD+: QM/MM Simulation of the Enzyme Reaction (2006) (10)
Novel enantioselective synthesis of (2S,2′R,3′R)-2-(2′,3′-dicarboxycyclopropyl)glycine (DCG-IV) (2000) (10)
Charting the Chemical Space of Target Sites: Insights into the Binding Modes of Amine and Amidine Groups (2009) (10)
Definition of a pharmacophore for the metabotropic glutamate receptors negatively linked to adenylyl cyclase. (1993) (10)
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A new amino acid derivative of ursodeoxycholate, (N-L-Glutamyl)-UDCA (UDCA-Glu), to selectively release UDCA in the colon. (2009) (9)
Homology model of the closed, functionally active, form of the amino terminal domain of mGlur1. (2001) (9)
Metabotropic glutamate receptors: a structural view point. (2000) (9)
Synthesis of 2-azabicyclo[3.1.0]hexane tricarboxylate and its transformation into a new proline-γ-acetic acid equivalent (1994) (9)
Preparation and physicochemical properties of natural (23R)-3α,7α,23- and (23R)-3α,12α,23-trihydroxylated bile acids and their (23S)-epimers (1989) (8)
Asymmetric synthesis of enantiomerically pure (2S,1'S,2'S,3'R)-phenylcarboxycyclopropylglycine (PCCG-4): A potent and selective ligand at group II metabotropic glutamate receptors (1996) (8)
Binding modes of noncompetitive AMPA antagonists: a computational approach. (2003) (8)
Characterization of d-3,4-cyclopropylglutamates as N-methyl-d-aspartate receptor agonists (1990) (8)
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Synthesis of all four diastereoisomers of 4-(carboxymethyl)proline, a conformationally constrained analogue of 2-aminoadipic acid (1995) (8)
Conformational properties of cholic acid, a lead compound at the crossroads of bile acid inspired drug discovery† (2014) (8)
Evaluation of hydrophobic/hydrophilic balance of bile acids by comparative molecular field analysis (CoMFA) (2000) (8)
3. Life or death decisions: the cast of poly(ADP-ribose)polymerase (PARP) as a therapeutic target for brain ischaemia. (2004) (8)
TGR 5 reduces macrophage migration through mTOR-induced C / EBP b differential translation (2018) (8)
Interfacial properties of most monofluorinated bile acids deviate markedly from the natural congeners: studies with the Langmuir-Pockels surface balance. (2005) (8)
1-Methyl-1-dihalomethylcyclohexane derivatives (1977) (7)
Homogeneous catalysis of the decomposition of dimethyl diazomalonate in alcohols (1977) (7)
C(15) configuration of isopimarene-15,16-diols (1980) (7)
Towards New Neuroprotective Agents: Design and Synthesis of 4H-Thieno[2,3-c]isoquinolin-5-one Derivatives as Potent PARP-1 Inhibitors. (2004) (7)
Drug Modeling at Cell Membrane Receptors: The Concept of Pseudoreceptors (1992) (7)
Metabotropic glutamate receptors coupled to phospholipase D (1996) (7)
Thermal and catalytic reactions of ethyl diazopyruvate with [60]fullerene (2010) (7)
The Discovery of Obeticholic Acid (Ocaliva™): First‐in‐Class FXR Agonist (2018) (7)
From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. (2020) (7)
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Catalysed insertion reactions of diphenyl diselenide with ethyl diazoacetate and dimethyl diazomalonate (1979) (7)
Molecular dynamics simulation of the ligand binding domain of mGluR1 in response to agonist and antagonist binding (2002) (7)
Synthesis and preliminary biological evaluation at the glycineB site of (+)- and (-)-3-oxetanylglycine, novel non-proteinogenic amino acids. (2001) (7)
Leaf pigments of Lycium europaeum: seasonal effect on zeaxanthin and lutein formation. (1969) (6)
Weak Microbial Metabolites: a Treasure Trove for Using Biomimicry to Discover and Optimize Drugs (2020) (6)
Alternative strategies for targeting mouse double minute 2 activity with small molecules: novel patents on the horizon? (2011) (6)
Cyclobutanones via the (1-Oxycyclopropyl)methanol Route (1977) (6)
Innovations and emerging therapies to combat renal cell damage: NAD+ as a drug target. (2021) (6)
Exploring the metal-catalyzed reaction of furans with alkyl α-diazomethanesulfonate and α-diazomethanephosphonate: synthesis of ω-acyl-substituted sulfono- and phosphonobutadienes (2009) (6)
A NEW SYNTHESIS OF DIETHYL ETHOXYMALONATE (1975) (6)
Metabotropic glutamate receptors: targets for therapy of cerebral ischaemia (2001) (6)
Syntheses of Compounds Active toward Glutamate Receptors: II. Synthesis of Spiro Hydantoins of the Indan Series (2002) (6)
The rearrangement of isothiochroman sulphonium ylides via a thermal ylide exchange reaction (1977) (6)
Synthesis, absolute configuration and activity at N-methyl-D-aspartic acid (NMDA) receptor of the four D-2-amino-4,5-methano-adipate diastereoisomers. (1991) (6)
Synthesis and chromatographic resolution of conformationally constrained analogues of homotaurine (2009) (5)
Dominant Factors Affecting the Chromatographic Behaviour of Bile Acids (2006) (5)
Synthesis and biological evaluation of 6-carboxy-3,4-methanoprolines, new rigid glutamate analogs. (1995) (5)
Structure of metal–carbenoid intermediates derived from the dirhodium(II)tetracarboxylate mediated decomposition of α-diazocarbonyl compounds: a DFT study (2002) (5)
Acid-catalysed decomposition of β,γ-unsaturated diazo-ketones preparation of 4,4-dimethyl-D-nor-steroidal systems from pimaradiene and sandaracopimaradiene precursors (1980) (5)
The structure of gelsevirine (1972) (5)
A partial homo-Favorskii rearrangement in the diterpene series (1982) (4)
Synthesis and Quantitative Structure-Property Relationships of Side Chain-Modified Hyodeoxycholic Acid Derivatives (2013) (4)
Photolysis of α-diazo carbonyl compounds in the presence of imidazole. A new method for the preparation of nor olefins and its application to bile acid side chain degradation (1984) (4)
Reductions of diterpene epoxides. A partial synthesis of 8.beta.-hydroxyisopimar-15-ene (1982) (4)
Synthesis of 6-methoxy-6a-hydroxymethylpenems (1995) (4)
Synthesis, preliminary evaluation and molecular modeling studies of new, conformationally constrained analogues of the competitive NMDA receptor antagonist 4-(phosphonomethyl)-2-piperidinecarboxylic acid (CGS 19755). (1997) (4)
Molecular Modeling of the Ligand-Binding Domains of the NR3A and NR3B Subunits of the NMDA Receptor (2003) (4)
Synthesis of 6,6-dicarboxy-3,4-methano-L-proline, a new constrained glutamate analog endowed with neuroprotective properties. (1996) (4)
Targeting the MDM 2 / MDM 4 Interaction Interface as a Promising Approach for p 53 Reactivation Therapy (2015) (4)
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Synthesis of 6β-methoxy-6α-hydroxymethylpenems (1995) (4)
3α-6α-Dihydroxy-7α-fluoro-5β-cholanoate (UPF-680), physicochemical and physiological properties of a new fluorinated bile acid that prevents 17α-ethynyl-estradiol-induced cholestasis in rats (2006) (4)
L-α-Aminoadipic Acid from L-Glutamic Acid (1988) (3)
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. (2019) (3)
1114 FUNCTIONAL CHARACTERIZATION OF THE SEMI-SYNTHETIC BILE ACID DERIVATIVE INT-767, A DUAL FXR AND TGR5 AGONIST (2010) (3)
Ablation of liver Fxr results in an increased colonic mucus barrier in mice (2021) (3)
Carbon-13 nuclear magnetic resonance spectroscopy of naturally occurring substances. 73. C(15) configuration of isopimaren-15,16-diols and sandaracopimaren-15,16-diols (1981) (3)
The preparation of d-norsteroidal skeletal type from a diterpenic precursor (1979) (3)
First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53 (2021) (3)
De novo NAD+ synthesis enhances mitochondrial function and improves health (2018) (3)
Effect of intraduodenal administration of 23-methyl-UDCA diastereoisomers on bile flow in hamsters (1992) (3)
23-Methyl-3 alpha,7 beta-dihydroxy-5 beta-cholan-24-oic acid: dose-response study of biliary secretion in rat. (1988) (3)
KYNURENINE-3-HYDROXYLASE AND ITS SELECTIVE INHIBITORS (1996) (3)
Comparative Analysis of the Ligand-Binding Sites of the Metabotropic Glutamate Receptors mGluR1–mGluR8 (2002) (3)
5-ASA-glutamate protects rats from inflammatory bowel disease induced by intracolonic administration of trinitrobenzensulfonic acid. (1998) (3)
Tetracyclic diterpenoids by intramolecular C-alkylation of γδ-unsaturated diazo ketones (1978) (3)
Farnesoid X receptor activation by the novel agonist TC-100 (3α, 7α, 11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid) preserves the intestinal barrier integrity and promotes intestinal microbial reshaping in a mouse model of obstructed bile acid flow. (2022) (3)
NMDA receptor heterogeneity in mammalian tissues: focus on two agonists, (2S,3R,4S) cyclopropylglutamate and the sulfate ester of 4-hydroxy-(S)-pipecolic acid (1995) (3)
Chromatographic separation and evaluation of the lipophilicity by reversed-phase high-performance liquid chromatography of fullerene-C60 derivatives (1999) (3)
FXR Promotes Adipocyte Differentiation and regulates adipose cell function in vivo (2006) (3)
The involvement of metabotropic glutamate class I receptors in LTP depends on tetanization strength (1996) (3)
BF3·Et2O‐Induced Decomposition of Ethyl 2‐Diazo‐3‐hydroxy‐3,3‐diarylpropanoates in Acetonitrile: A Novel Approach to 2,3‐Diaryl β‐Enamino Ester Derivatives. (2009) (2)
BILE ACIDS WITH CYCLOPROPANE-CONTAINING SIDE CHAIN. 2. SYNTHESIS AND PROPERTIES OF 3α,7β-DIHYDROXY-22,23-METHYLENE-5β-CHOLAN-24-OIC ACID (2-SULFOETHYL)AMIDE (1985) (2)
Stereospecific Synthesis of the Enantiomers of Nicotinylalanine, a Neuroprotecting Agent. (1992) (2)
Syntheses of Compounds Active toward Glutamate Receptors: I. New Preparative Synthesis of Aminoindandicarboxylic Acid (AIDA) (2002) (2)
Adamantane derivatives of biological interest. Synthesis and antiviral activity of 2-(1-adamantyl)imidazole derivatives. (1981) (2)
Heterocyclic modulators of the NMDA receptor. (1993) (2)
New One-Pot Synthesis of Pyrazole-5-carboxylates by 1,3-Dipole Cycloadditions of Ethyl Diazoacetate with α-Methylene Carbonyl Compounds. (2010) (2)
3alpha-6alpha-Dihydroxy-7alpha-fluoro-5beta-cholanoate (UPF-680), physicochemical and physiological properties of a new fluorinated bile acid that prevents 17alpha-ethynyl-estradiol-induced cholestasis in rats. (2006) (2)
CONVERSION OF VIRESCENOL A INTO VIRESCENOL B (1977) (2)
BF3·Et2O-Promoted Decomposition of Cyclic α-Diazo-β-Hydroxy Ketones: Novel Insights into Mechanistic Aspects (2018) (2)
S.09.03 Group 1 and group 2 metabotropic glutamate receptor agents: Pharmacological studies in vitro and in vivo (1997) (2)
Synthesis and Activity of Enantiopure (S) (m‐Nitrobenzoyl)alanine, a Potent Kynurenine‐3‐hydroxylase Inhibitor. (1995) (2)
SOLVOLYSIS OF VIRESCENOL B 19-TOSYLATE (1978) (2)
Molecular Modeling of the mGluR1 Metabotropic Glutamate Receptor Transmembrane Domain and Construction of the Model of Its Dimer (2003) (2)
Synthesis of Novel Unsymmetrically Bridgehead-Substituted Phenylselenobicyclo[1.1.1]pentanes. (2004) (1)
Synthesis and receptor binding affinity of cholecystokinin receptor ligands: 2-and 1-indolyl derivatives of PD134308. (1996) (1)
Tu1898 Therapeutic Potential of a Novel Poly(ADP-ribose) Polymerase Inhibitor, Hydamtiq, in Human Pancreatic and Colon Cancers (2013) (1)
Dominant Factors Affecting the Chromatographic Behaviour of Bile Acids (2006) (1)
Synthesis and Preliminary Biological Evaluation at the GlycineB Site of (+)‐ and (‐)‐3‐Oxetanylglycine, Novel Non‐proteinogenic Amino Acids. (2002) (1)
Liver-gut axis controls the colonic mucus barrier via hepatic FXR (2021) (1)
Rhodium-Catalyzed Redox Isomerization of Hydroxy Alkynes to trans keto and Hydroxy Vinyl Esters. A Short and Stereoselective Synthesis of Dipeptide Isosters. (1995) (1)
Synthesis of Methano[60]fullerenephosphonic- and Methano[60]fullerenediphosphonic Acids (2000) (1)
The neuroprotective activity of group-II mGlu receptor agonist is sensitive to protein synthesis inhibitors and involves the interaction between neurons and astrocytes (1996) (1)
Conformationally Constrained Tryptophan Analogues. Synthesis of (.+-.)- (Z)- and (.+-.)-(E)-2-Amino-2,3-methano-3-(indol-3-yl)-propanoic Acids (1996) (1)
RING EXPANSION OF THIOCHROMAN-4-ONE AND ISOTHIOCHROMAN-4-ONE WITH ETHYL DIAZO(LITHIO)ACETATE TO TETRAHYDROBENZOTHIEPIN β-OXOESTERS (1977) (1)
UPF 996 activates mGluR5 but not mGluR1 in brain slices and modulates excitability of CA1 pyramidal cells (1998) (1)
Indole and quinoline derivatives of 2,3‐dihydro‐l‐benzothiepin‐4(5H) one (1978) (1)
The FXR-agonist, 6-ethyl-chenodeoxycholic acid (6-ECDCA), protects against estrogen-induced cholestasis in rats (2003) (1)
Synthesis of Methano[60]fullerenephosphonic- and Methano[60]fullerene-diphosphonic Acids. (2001) (1)
Structural Basis of Human Dimeric α-Amino-β-Carboxymuconate-ε-Semialdehyde Decarboxylase Inhibition With TES-1025 (2022) (1)
カルボキシテルフェナジン(フェキソフェナジン)とその生物的同配体のテトラゾール類似体の新しい合成法 (1999) (1)
Insights into Phenylalanine Derivatives Recognition of VLA‐4 Integrin: From a Pharmacophoric Study to 3D‐QSAR and Molecular Docking Analyses. (2004) (1)
Chapter 10:TGR5 Agonists in Development (2012) (1)
Molecular Modeling of the Closed Forms of the Kainate-Binding Domains of Kainate Receptors and Qualitative Analysis of the Structure–Activity Relationships for Some Agonists (2002) (1)
Synthesis of 2-Azabicyclo(3.1.0)hexane Tricarboxylate and Its Transformation into a New Proline-γ-acetic Acid Equivalent. (1994) (1)
Synthesis of Novel Unsymmetrically Bridgehead-substituted Phenylselenobicyclo[1.1.1]pentanes (2004) (1)
THE PREPARATION OF A 4,4-DIMETHYL-15-OXA STEROID (1982) (1)
Metabolically stable analogs of ursodeoxycholic acid inhibit colonic epithelial secretion in vitro and in vivo (2010) (0)
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Metabotropic Glutamate Receptors: Structure and New Subtype‐Selective Ligands (2001) (0)
Unsaturated derivatives of bile acids, process for their preparation and pharmaceutical compositions containing them. (1991) (0)
Effects of Molecular Dynamics and Replica Exchange Molecular Dynamics in Sampling the Conformational Space of PARP-1 (2013) (0)
Chromatographic Separation and Evaluation of the Lipophilicity by RP-HPLC of Fullerene C60 Derivatives (1999) (0)
Carboxyfullerens reduce apoptotic death induced in cultured human keratinocytes by ultraviolet radiation (1998) (0)
THE SYNTHESIS OF A CYCLOPROPYL GALACTOPYRANOSIDE (1984) (0)
HOMOLYTIC SUBSTITUTION AND CARBENOIDIC REACTIONS IN THE PREPARATION OF BENZIMIDAZOLE DERIVATIVES OF PHARMACEUTICAL INTEREST: SYNTHESIS AND PROPERTIES OF (2-CYCLOALKYL-1-BENZIMIDAZOLYL)-N,N-DIETHYLACETAMIDES (1985) (0)
Biliary acid derivative, its production and medicinal composition containing the same (1988) (0)
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Procede de reduction d'effets secondaires indesirables induits par un medicament chez un patient (2005) (0)
Conformational requirements for interaction of L-glutamate with the metabotropic EAA receptor (1993) (0)
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Synthesis of All Four Diastereoisomers of 4‐(Carboxymethyl)proline, a Conformationally Constrained Analogue of 2‐Aminoadipic Acid. (1995) (0)
Structural Basis for 3-deoxy-CDCA Binding and Activation of FXR (2004) (0)
Modulation of glutamate receptors in search of protection from excitotoxic-induced neuron death (1999) (0)
D-3,4-′Cyclopropylglutamate′ Isomers as NMDA Receptor Ligands: Synthesis and Enantioselective Activity. (1990) (0)
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Pharmacological studies on new agonists and antagonists of mGluRs (1996) (0)
Targeting TGR5 in diabesity: Focus on S-EMCA (INT-777) a potent and selective bile acid mimetic agonist (2010) (0)
Derivatives of thieno, 2, 3-c | isoquinolin-3-one as inhibitors of poly (dp-ribose) polymerase (2000) (0)
A process for the preparation of bile acid derivatives (2013) (0)
Insights in the PARP1 poisoning effect (2013) (0)
FXR agonist new steroid. (2005) (0)
PREPARATION OF ETHYL 4-OXO-TETRAHYDROBENZOXEPIN-5-CARBOXYLATES, BY RING EXPANSION OF CHROMAN-4-ONE AND ISOCHROMAN-4-ONE WITH ETHYL DIAZO(LITHIO)ACETATE, AND THEIR DECARBOXYLATION TO DIHYDROBENZOXEPINONES (1979) (0)
S.28.02 Astrocytes, kynurenic acid and schizophrenia: multiple emerging links (2007) (0)
INDOLE AND QUINOLINE DERIVATIVES OF 2,3-DIHYDRO-1-BENZOTHIEPIN-4(5H)-ONE (1979) (0)
Sulfur-containing bile acid derivatives (1993) (0)
Enantiospecific Synthesis of a Chiral Carbapenem Precursor from (R)-Aspartic Acid. (1987) (0)
Cyclopropyl Dafachronic Acid Stereoisomers as Conformationally Constrained DAF-12 Ligands (2015) (0)
REACTIONS OF α-CYCLOCITRAL WITH ETHYL DIAZO(LITHIO)ACETATE AND WITH 1-DIAZO-1-LITHIOACETONE (1979) (0)
ATYPICAL BILE ACIDS AS CHEMICAL PROBES FOR DIAGNOSIS AND THERAPHY MONITORING OF PROGRESSIVE CHOLESTATIC LIVER DISEASE IN HSD3B7 PATIENTS (2016) (0)
Development of an Efficient continuous flow synthesis of glyco- and tauro-conjugated natural and semi-synthetic bile acids (2011) (0)
Derivatives of bile acids, process for their preparation and related pharmaceutical compositions (1982) (0)
Drug Discovery: Back and Forward (2004) (0)
Indium Triflate Catalyzed Reaction of Diisopropyl Diazomethylphosphonate with Imines as a New Approach to cis- and trans-Aziridine-2-phosphonates. (2007) (0)
Asymmetric Synthesis of Enantiomerically Pure (2S,1′S,2′S,3′R)- Phenylcarboxycyclopropylglycine (PCCG-4): A Potent and Selective Ligand at Group II Metabotropic Glutamate Receptors. (1997) (0)
L-α-Aminoadipic Acid from L-Glutamic Acid. (1989) (0)
Kynurenine-3-hydroxylase and its selective inhibitors. Molecular modeling studies. (1996) (0)
ACID-CATALYZED DECOMPOSITION OF β,Γ-UNSATURATED DIAZO-KETONES: PREPARATION OF 4,4-DIMETHYL-D-NORSTEROIDAL SYSTEMS FROM PIMARADIENE AND SANDARACOPIMARADIENE PRECURSORS (1980) (0)
Process for the preparation of 3-to-ya acids (b) dihydroxy-6-a (b) -alkyl-5b-colanici (2005) (0)
mGluRs novel ligands and molecular modeling studies (1996) (0)
bile acid 23-substituted as TGR5 modulators and methods of use thereof (2008) (0)
Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells. (2022) (0)
Synthesis and biological activity of cyclopropyl Δ7-dafachronic acids as DAF-12 receptor ligands. (2021) (0)
PREPARATION OF 1-(AROYLALKYL)-1H-IMIDAZOLE AND -BENZIMIDAZOLE DERIVATIVES OF PHARMACEUTICAL INTEREST. A NEW SYNTHETIC PROCEDURE (1984) (0)
Bile acid derivatives as FXR ligands for the prevention or treatment of diseases or conditions mediated by FXR (2007) (0)
Preparation and Physicochemical Properties of Natural (23R)-3α,7α,23- and (23R)-3α,12α,23-Trihydroxylated Bile Acids and Their (23S)-Epimers. (1989) (0)
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Heterocycles as Companions on Route to Drug Discovery (2002) (0)
The preparation of 5-spiro-7'-(bicyclo (4.1.0.) heptane)barbituric acid. (1976) (0)
SYNTHESIS OF 6BETA -METHOXY-6ALPHA -HYDROXYMETHYLPENEMS (1995) (0)
Molecular Dynamic Simulation of the Ligand–Receptor Complexes of the Aminoterminal Domain of the Metabotropic Glutamate Receptor mGluR1 (2003) (0)
Homology modeling of mGluR1 ATD reveals different modes of binding of mGluR1 agonists and antagonists (1996) (0)
Inhibiteurs de la semialdehyde decarboxylase de l'acide alpha-amino-beta-carboxymuconique (2015) (0)
Targeting the Conformational Transitions of MDM2 and MDMX.PART II: Insights into Key Residues Affecting p53 Recognition. (2008) (0)
A NEW SYNTHESIS OF β-DAMASCONE (1981) (0)
N-L-glutamyl-UDCA as prodrug for colon-specific drug delivery (2000) (0)
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Design, Synthesis and Preliminary Evaluation of Novel 3′-Substituted Carboxycyclopropylglycines (XIV) as Antagonists at Group 2 Metabotropic Glutamate Receptors. (2002) (0)
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Synthesis and Preliminary Biological Evaluation of (2S,1′R,2′S)‐ and (2S,1′S,2′R)‐2‐(2′‐Phosphonocyclopropyl)glycines, Two Novel Conformationally Constrained L‐AP4 Analogues. (2006) (0)
Molecular modeling of the transmembrane domain of the metabotropic glutamate receptor mGluR1 and the model of its dimeric form (2003) (0)
(S)-(-)-alpha,alpha-Di(2-naphthyl)-2-pyrrolidinemethanol, a useful tool to study the recognition mechanism in chiral ligand-exchange chromatography. (2007) (0)
Targeting the FXR nuclear receptor through a virtual screening approach (2011) (0)
Amino acid derivatives of UDCA as novel prodrugs for colon-specific drug delivery (2000) (0)
Effect of novel mGluR antagonists on signal transduction in mesencephalic and striatal neurons in vitro (1996) (0)
New insights into the evaluation of the bile salt critical micellar concentration (2008) (0)
A New Synthesis of 6‐Oxopenicillanates by Ozonolysis of 6‐ Diazopenicillanates. (1992) (0)
Exploring the Metal-Catalyzed Reactions of Furans with Alkyl α-Diazomethanesulfonate and α-Diazomethanephosphonate: Synthesis of ω-Acyl-Substituted Sulfono- and Phosphonobutadienes. (2009) (0)
5-aminosalicylsäurederivate for therapy of chronic inflammatory diseases belly. (1991) (0)
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Design, synthesis, molecular modeling and biological activity of chenodeoxycholic acid carbamate derivatives as potent and selective FXR agonists (2010) (0)
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Homology Modeling of AMPA Receptors: Route to the identification of noncompetitive antagonists binding site (2002) (0)
PARP Inhibitors As Anticancer Agents (2010) (0)
SCALE-UP SYNTHESIS OF 3α,7α,23-TRIHYDROXY-6α-ETHYL-24-NOR-5β-CHOLAN-23-SULFATE SODIUM SALT (INT-767), A POTENT FXR/TGR5 DUAL AGONIST IN PHASE I CLINICAL STUDIES (2016) (0)
Design and structure-activity/selectivity in NMDA receptor agonists and antagonists (1990) (0)
THEORETICAL MODEL OF METABOTROPIC GLUTAMATE RECEPTOR MGLUR3 IN OPEN FORM (2004) (0)
Synthesis of 6a-methoxy-6-hydroxymethylpenems (1996) (0)
The methyl trasnferase PRMT1 functions as coactivator of FXR/RXR and regulates transcription of FXR responsive genein hepatocytes (2004) (0)
Interfacial properties of most monofluorinated bile acids deviate markedly from the natural congeners Published, JLR Papers in Press, December 16, 2004. DOI 10.1194/jlr.M400439-JLR200 (2005) (0)
Structure-activity studies on kynurenates (1990) (0)
Derivatives of 5-aminosalicylic acid for the therapy of chronic inflammatory diseases of the intestine. (1991) (0)
Gallensaeurederivate, processes for their preparation and compositions containing them pharmaceutical. (1984) (0)
[Derivatives of isothiochromane]. (1975) (0)
REDUCTION OF α-DIAZO-β-HYDROXY ESTERS TO β-HYDROXY ESTERS: APPLICATION IN ONE OF TWO CONVERGENT SYNTHESIS OF A (22S)-22-HYDROXY BILE ACID FROM FISH BILE AND ITS (22R)-EPIMER (1985) (0)
Quinolinic and kynurenic acids content and their regulation in the rat brain and other organs (1990) (0)
Novel 1,4-Dihydropyridine Derivatives as Mineralocorticoid Receptor Antagonists (2023) (0)
Procede d'elaboration d'acide 3alpha(beta)-7alpha(beta)-dihydroxy-6alpha(beta)-alkyle-5beta-cholanique (2006) (0)
Structure-activity studies on thiol derivatives of kynurenic acid (1990) (0)
Bile acid derivatives, processes for preparation thereof and compositions containing them pharmaceutical. (1988) (0)
Synthesis and Preliminary Evaluation of (S)‐2‐(4′‐Carboxycubyl)glycine, a New Selective mGluR1 Antagonist. (1998) (0)
Unsaturated bile acid derivatives, to processes for their preparation and to pharmaceutical compositions containing them (1991) (0)
Pharmacological studies on agonists and antagonists of metabotropic glutamate receptors (1995) (0)
The Reaction of α-Diazo-β-hydroxy Esters with Boron Trifluoride. (1994) (0)
Dehydroxylation-Resistant Derivatives of Ursodeoxycholic Acid: A New Approach to Treating Secretory Diarrheal Diseases? (2011) (0)
BICYCLO(3,2,0)HEPTANOLS (1974) (0)
9. The Systems Biology of Transporters – Targeting the Regulatory System for Transporters (FXR/RXR) (2017) (0)
α-Diazocarbonyl Chemistry - Target Driven Applications (1998) (0)
Metabotropic glutamate receptors: a structural view point (2000) (0)
Concepts and Molecular Aspects in the Polypharmacology of PARP-1 Inhibitors (2016) (0)
Bile acid derivatives, processes for their preparation and pharmaceutical compositions containing them. (1988) (0)
Short Communication (S)-(-)-a,a-Di(2-naphthyl)-2-pyrrolidinemethanol, a useful tool to study the recognition mechanism in chiral ligand-exchange chromatography (2007) (0)
Side chain modified HDCA derivatives: synthesis, CMC determination and molecular modelling studies. (2013) (0)
Dirhodium(II) Tetraacetate‐Mediated Decomposition of Ethyldiazoacetate and Ethyldiazomalonate in the Presence of Fullerene. A New Procedure for the Selective Synthesis of [6‐6]‐Closed Methanofullerenes. (1998) (0)
7,8-ISOPIMARENIC EPOXIDES: PREPARATION AND ACID-CATALYZED RING CLEAVAGE (1981) (0)
PHOTOLYSIS OF α-DIAZO CARBONYL COMPOUNDS IN THE PRESENCE OF IMIDAZOLE. A NEW METHOD FOR THE PREPARATION OF NOROLEFINS AND ITS APPLICATION TO BILE ACI SIDE CHAIN DEGRADATION (1984) (0)
Cover Picture: Modulators of the Kynurenine Pathway of Tryptophan Metabolism: Synthesis and Preliminary Biological Evaluation of (S)‐4‐(Ethylsulfonyl)benzoylalanine, a Potent and Selective Kynurenine Aminotransferase II (KAT II) Inhibitor (ChemMedChem 5/2006) (2006) (0)
Fluorinated bile acid derivatives, processes for their preparation and pharmaceutical compositions thereof. (1990) (0)
T1818 Metabolically Stable Analogs of Ursodeoxycholic Acid: A New Class of Anti-Diarrheal Drug? (2010) (0)
Antonio Structural Changes SHP Associated with Functional and Novel Polymorphisms of Nuclear Receptor Molecular Bases of Disease (2010) (0)
Kynurensäurederivate, their preparation and pharmaceutical compositions containing them. (1990) (0)
Synthesis of 3beta,7alpha-Dihydroxy-Δ5-cholenoic Acid Derivatives: ‘Atypical’ Bile Acid Metabolites and Useful Biomarkers to Detect 3delta-HSDH Deficiency (2013) (0)
Halogenthienoylcyclopropan-1-carboxylic acid derivatives (2003) (0)
Farnesoid-X-receptor (FXR) ligands induce a small heterodimer partner (SHP)-dependent upregulation of PPAR-gamma in hepatic stellate cells and in rat model of liver fibrosis. (2004) (0)
Eco-sustainable Synthesis of Bioactive Sulfonamides: from Batch to Flow Approach (2012) (0)
Thermal and Catalytic Reaction of Diazoacetylmetallocenes with [60]Fullerene. (2003) (0)
β-KETO ESTERS FROM THE RHODIUM(II) ACETATE CATALYZED CONVERSION OF α-DIAZO-β-HYDROXY ESTERS (1980) (0)
Garcinoic AcidIs a Natural and Selective Agonistof Pregnane X Receptor (2020) (0)
Mo1915 Novel Wnt-Targeted Therapy Inhibitors for Hepatocellular Carcinoma (2014) (0)
Development of 3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites. (2022) (0)
Modification of ITP by metabotropic glutamate class I receptor activation or inhibition in vitro (1996) (0)

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