Synthesis and multiparametric evaluation of thiadiazoles and oxadiazoles as diacylglycerol acyltransferase type 1 inhibitors

Autor:	Philippe Péron, Marie-Aude Chabanaud, Gwladys Langot, Etienne Guillot, Florence Goumy, Patrick Mougenot, Cecile Pascal, Olivier Crespin, Fabrice Viviani, Majdi Ben-Hassine, Friedemann Schmidt, Eykmar Fett, Jean-Christophe Le Bail, Jean-Luc Ragot, Bénédicte Onofri, Rommel Dadji-Faïhun, Christophe Philippo, Thao Van-Pham, Catherine Monseau, Olivier Venier, Jerome Menegotto, Florence Chatelain-Egger, Marie-Pierre Pruniaux, François Pacquet, Philippe Chamiot-Clerc, Eric Nicolai, Claudie Namane
Rok vydání:	2016
Předmět:	Models Molecular 0301 basic medicine Clinical Biochemistry Pharmaceutical Science Oxadiazole 01 natural sciences Biochemistry Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Diacylglycerol O-Acyltransferase Thiadiazoles Drug Discovery Humans Molecule Structure–activity relationship Enzyme Inhibitors Solubility Molecular Biology Oxadiazoles Dose-Response Relationship Drug Molecular Structure Organic Chemistry 0104 chemical sciences 010404 medicinal & biomolecular chemistry 030104 developmental biology chemistry Molecular Medicine Diacylglycerol Acyltransferase
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 26:25-32
ISSN:	0960-894X
Popis:	Chemical modulation of a formerly disclosed DGAT-1 inhibitor resulted in the identification of a compound with a suitable profile for preclinical development. Optimisation of solubility is discussed and a PK/PD study is presented.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ccd83610869fd9f5432e155ed4fbc2f https://doi.org/10.1016/j.bmcl.2015.11.046 Zobrazit plný text záznamu Full Text from ScienceDirect