Ontology highlight
ABSTRACT:
SUBMITTER: Cheung M
PROVIDER: S-EPMC5807866 | biostudies-other | 2018 Feb
REPOSITORIES: biostudies-other
Cheung Mui M Tangirala Raghuram S RS Bethi Sridhar R SR Joshi Hemant V HV Ariazi Jennifer L JL Tirunagaru Vijaya G VG Kumar Sanjay S
ACS medicinal chemistry letters 20180116 2
Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) plays an important role in triglyceride synthesis and is a target of interest for the treatment of metabolic disorders. Herein we describe the structure-activity relationship of a novel tetralone series of DGAT1 inhibitors and our strategies for overcoming genotoxic liability of the anilines embedded in the chemical structures, leading to the discovery of a candidate compound, (<i>S</i>)-2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyrazin-2-yl)-1-oxo-2 ...[more]