title: Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1.
abstract: A novel class of DGAT1 inhibitors containing a thiadiazole core has been discovered. Chemical optimization lead to inhibitors of human DGAT1 with an appropriate ADME profile and that show in vivo activity in target tissues.
authors.affiliation: Sanofi-aventis R&D, Early to Candidate Unit, 1 avenue Pierre Brossolette, 91385 Chilly-Mazarin, France. patrick.mougenot@sanofi-aventis.com
authors.forename: Patrick
authors.initials: P
authors.lastname: Mougenot
authors.forename: Claudie
authors.initials: C
authors.lastname: Namane
authors.forename: Eykmar
authors.initials: E
authors.lastname: Fett
authors.forename: Florence
authors.initials: F
authors.lastname: Camy
authors.forename: Rommel
authors.initials: R
authors.lastname: Dadji-Faïhun
authors.forename: Gwladys
authors.initials: G
authors.lastname: Langot
authors.forename: Catherine
authors.initials: C
authors.lastname: Monseau
authors.forename: Bénédicte
authors.initials: B
authors.lastname: Onofri
authors.forename: François
authors.initials: F
authors.lastname: Pacquet
authors.forename: Cécile
authors.initials: C
authors.lastname: Pascal
authors.forename: Olivier
authors.initials: O
authors.lastname: Crespin
authors.forename: Majdi
authors.initials: M
authors.lastname: Ben-Hassine
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Ragot
authors.forename: Thao
authors.initials: T
authors.lastname: Van-Pham
authors.forename: Christophe
authors.initials: C
authors.lastname: Philippo
authors.forename: Florence
authors.initials: F
authors.lastname: Chatelain-Egger
authors.forename: Philippe
authors.initials: P
authors.lastname: Péron
authors.forename: Jean-Christophe
authors.initials: JC
authors.lastname: Le Bail
authors.forename: Etienne
authors.initials: E
authors.lastname: Guillot
authors.forename: Philippe
authors.initials: P
authors.lastname: Chamiot-Clerc
authors.forename: Marie-Aude
authors.initials: MA
authors.lastname: Chabanaud
authors.forename: Marie-Pierre
authors.initials: MP
authors.lastname: Pruniaux
authors.forename: Friedemann
authors.initials: F
authors.lastname: Schmidt
authors.forename: Olivier
authors.initials: O
authors.lastname: Venier
authors.forename: Eric
authors.initials: E
authors.lastname: Nicolaï
authors.forename: Fabrice
authors.initials: F
authors.lastname: Viviani
mesh_terms: D018938:Caco-2 Cells; D002986:Clinical Trials as Topic; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014280:Triglycerides / Q000037:antagonists & inhibitors* / Q000096:biosynthesis
chemical_list: D004791:Enzyme Inhibitors; D007004:Hypoglycemic Agents; D013830:Thiadiazoles; D014280:Triglycerides; C494881:DGAT1 protein, human; D051048:Diacylglycerol O-Acyltransferase