Search Results - "VOUY LINH TRUONG"
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Studies Directed toward Asymmetric Synthesis of Cardioactive Steroids via Anionic Polycyclization
Published in Organic letters (26-12-2002)“…The use of anionic polycyclization (AP) in constructing the steroidal backbone of cardenolides was investigated. The reaction of 2-carbomethoxy-2-cyclohexenone…”
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Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors
Published in Journal of lipid research (01-01-2016)“…Lipids are used as cellular building blocks and condensed energy stores and also act as signaling molecules. The glycerolipid/ fatty acid cycle, encompassing…”
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The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K
Published in Bioorganic & medicinal chemistry (01-02-2008)“…Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724…”
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Synthesis of a novel peptidic photoaffinity probe for the PTP-1B enzyme
Published in Bioorganic & medicinal chemistry letters (03-05-2004)“…The synthesis of a novel radioactive peptidic photoaffinity probe for the PTP-1B enzyme as well as some SAR leading to the choice of this compound as a…”
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Asymmetric Syntheses of 1-Aryl-2,2,2-trifluoroethylamines via Diastereoselective 1,2-Addition of Arylmetals to 2-Methyl-N-(2,2,2-trifluoroethylidene)propane-2-sulfinamide
Published in Organic letters (15-02-2007)“…Condensation of N-tert-butanesulfinamide (S)-1 with trifluoroacetaldehyde hydrate 2a afforded 2-methyl-N-(2,2,2-trifluoroethylidene)propane-2-sulfinamide 3…”
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Practical and efficient synthesis of N-fused tricyclic indoles
Published in Tetrahedron letters (05-01-2011)“…A practical and efficient synthesis of methyl 6,7,8,9-tetrahydropyrido[1,2-a]indol-10-ylacetate derivatives 6 is reported. This synthetic approach featured the…”
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Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group
Published in ACS medicinal chemistry letters (14-07-2016)“…A novel HIV protease inhibitor was designed using a morpholine core as the aspartate binding group. Analysis of the crystal structure of the initial lead bound…”
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Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y₁₄ receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-05-2011)“…A weak antagonist of the pyrimidinergic receptor P2Y₁₄ containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent…”
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The identification of potent, selective, and bioavailable cathepsin S inhibitors
Published in Bioorganic & medicinal chemistry letters (01-09-2007)“…The Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Qué., Canada H9H 3L1. Highly potent, selective, and bioavailable…”
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Identification of a potent and selective non-basic cathepsin K inhibitor
Published in Bioorganic & medicinal chemistry letters (01-04-2006)“…Based on our previous study with trifluoroethylamine as a P2–P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound…”
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Difluoroethylamines as an amide isostere in inhibitors of cathepsin K
Published in Bioorganic & medicinal chemistry letters (01-02-2011)“…The trifluoroethylamine group found in cathepsin K inhibitors like odanacatib can be replaced by a difluoroethylamine group. This change increased the basicity…”
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Mild and efficient ligand-free copper-catalyzed condensation for the synthesis of quinazolines
Published in Tetrahedron letters (27-01-2010)“…Condensation of o-iodobenzaldehydes 1a– c with amidine hydrochlorides 2a– p under ligand-free copper-catalyzed Ullmann N-arylation conditions afforded the…”
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Selective isolation of in vitro phase II conjugates using a lipophilic anionic exchange solid phase extraction method
Published in Journal of chromatography. B, Analytical technologies in the biomedical and life sciences (01-03-2008)“…Identification, characterization and structure elucidation of human metabolites of drug candidates is crucial for the pharmaceutical industry to assess their…”
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Rhodium-catalyzed diastereoselective 1,2-addition of arylboronic acids to chiral trifluoroethyl imine
Published in Tetrahedron letters (08-04-2009)“…Rhodium-catalyzed 1,2-addition of arylboronic acids 4a–j to chiral trifluoroethyl imine 3 afforded diastereomerically enriched sulfinamides 5a–j. The chiral…”
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Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)
Published in Journal of medicinal chemistry (22-02-2024)“…ATR is a key kinase in the DNA-damage response (DDR) that is synthetic lethal with several other DDR proteins, making it an attractive target for the treatment…”
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Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases
Published in Bioorganic & medicinal chemistry letters (01-01-2011)“…In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two…”
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The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat…”
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Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y sub(14 receptor antagonists)
Published in Bioorganic & medicinal chemistry letters (15-05-2011)“…A weak antagonist of the pyrimidinergic receptor P2Y sub(14 containing a dihydropyridopyrimidine core was identified through high-throughput screening…”
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Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y 14 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (2011)“…A weak antagonist of the pyrimidinergic receptor P2Y 14 containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent…”
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