Discovery of DF-461, a Potent Squalene Synthase Inhibitor.

ABSTRACT: We report the development of a new trifluoromethyltriazolobenzoxazepine series of squalene synthase inhibitors. Structure-activity studies and pharmacokinetics optimization on this series led to the identification of compound 23 (DF-461), which exhibited potent squalene synthase inhibitory activity, high hepatic selectivity, excellent rat hepatic cholesterol synthesis inhibitory activity, and plasma lipid lowering efficacy in nonrodent repeated dose studies.

SUBMITTER: Ichikawa M 

PROVIDER: S-EPMC4027440 | biostudies-literature | 2013 Oct

REPOSITORIES: biostudies-literature