about
Patented TGR5 modulators: a review (2006 - present).Determination of bile salt critical micellization concentration on the road to drug discovery.Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases.Synthesis and structure-activity relationships of amino acid conjugates of cholanic acid as antagonists of the EphA2 receptor.Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.Probing the Binding Site of Bile Acids in TGR5.TGR5-mediated bile acid sensing controls glucose homeostasisBack door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.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.Synthesis and quantitative structure-property relationships of side chain-modified hyodeoxycholic acid derivatives.First general approach to cyclohex-3-ene-1,1-bis(phosphonates) by Diels-Alder cycloaddition of tetraethyl vinylidenebis(phosphonate) to 1,3-dienes.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.Achiral-chiral two-dimensional chromatography of free amino acids in milk: A promising tool for detecting different levels of mastitis in cows.Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.Synthesis of atypical bile acids for use as investigative tools for the genetic defect of 3β-hydroxy-Δ(5)-C27-steroid oxidoreductase deficiency.Selected cholesterol biosynthesis inhibitors produce accumulation of the intermediate FF-MAS that targets nucleus and activates LXRα in HepG2 cells.Investigating the allosteric reverse signalling of PARP inhibitors with microsecond molecular dynamic simulations and fluorescence anisotropy.Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.Semisynthetic bile acid FXR and TGR5 agonists: physicochemical properties, pharmacokinetics, and metabolism in the ratMulticlass screening method to detect more than fifty banned substances in bovine bile and urineProgress and challenges of selective Farnesoid X Receptor modulationTandem 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 responseGlucuronidation of bile acids under flow conditions: design of experiments and Koenigs-Knorr reaction optimizationThermal and catalytic reactions of ethyl diazopyruvate with [60]fullereneContinuous Flow Synthesis of Thieno[2,3-c]isoquinolin-5(4H)-one Scaffold: A Valuable Source of PARP-1 InhibitorsExploring 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)acetateCorrelation between CMC and chromatographic index: simple and effective evaluation of the hydrophobic/hydrophilic balance of bile acidsMolecular dynamics simulation of the ligand binding domain of farnesoid X receptor. Insights into helix-12 stability and coactivator peptide stabilization in response to agonist bindingNovel stereoselective synthesis and chromatographic evaluation of E-guggulsteroneDerived chromatographic indices as effective tools to study the self-aggregation process of bile acidsContinuous flow synthesis and scale-up of glycine- and taurine-conjugated bile saltsSide-chain modified bile acids: chromatographic separation of 23-methyl epimersHPLC/ELSD analysis of amidated bile acids: an effective and rapid way to assist continuous flow chemistry processesChromatographic separation of free dafachronic acid epimers with a novel triazole click quinidine-based chiral stationary phaseFlow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitorsEnantioselective HPLC Analysis to Assist the Chemical Exploration of Chiral ImidazolinesThe Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow TechnologyGarcinoic Acid Is a Natural and Selective Agonist of Pregnane X ReceptorDissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool
P50
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