Ontology highlight
ABSTRACT:
SUBMITTER: He S
PROVIDER: S-EPMC4207266 | biostudies-literature | 2014 Oct
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20140908 10
We report the discovery of a novel series of DGAT1 inhibitors in the benzimidazole class with a piperdinyl-oxy-cyclohexanecarboxylic acid moiety. This novel series possesses significantly improved selectivity against the A2A receptor, no ACAT1 off-target activity at 10 μM, and higher aqueous solubility and free fraction in plasma as compared to the previously reported pyridyl-oxy-cyclohexanecarboxylic acid series. In particular, 5B was shown to possess an excellent selectivity profile by screeni ...[more]