Ontology highlight
ABSTRACT:
SUBMITTER: Zhou G
PROVIDER: S-EPMC4027756 | biostudies-literature | 2014 May
REPOSITORIES: biostudies-literature
Zhou Gang G Zorn Nicolas N Ting Pauline P Aslanian Robert R Lin Mingxiang M Cook John J Lachowicz Jean J Lin Albert A Smith Michelle M Hwa Joyce J van Heek Margaret M Walker Scott S
ACS medicinal chemistry letters 20140301 5
Diacylglycerol acyltransferase 1 (DGAT1) presents itself as a potential therapeutic target for obesity and diabetes for its important role in triglyceride biosynthesis. Herein we report the rational design of a novel class of DGAT1 inhibitors featuring a benzomorpholine core (23n). SAR exploration yielded compounds with good potency and selectivity as well as reasonable physical and pharmacokinetic properties. This class of DGAT1 inhibitors was tested in rodent models to evaluate DGAT1 inhibitio ...[more]