Ontology highlight
ABSTRACT:
SUBMITTER: Zhang X
PROVIDER: S-EPMC5430397 | biostudies-literature | 2017 May
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20170421 5
We have discovered a novel series of tetrahydrobenzimidazoles <b>3</b> as TGR5 agonists. Initial structure-activity relationship studies with an assay that measured cAMP levels in murine enteroendocrine cells (STC-1 cells) led to the discovery of potent agonists with submicromolar EC<sub>50</sub> values for mTGR5. Subsequent optimization through methylation of the 7-position of the core tetrahydrobenzimidazole ring resulted in the identification of potent agonists for both mTGR5 and hTGR5 (human ...[more]