Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

ABSTRACT: Hit-to-lead efforts resulted in the discovery of compound 19, a potent CYP11B2 inhibitor that displays high selectivity vs related CYPs, good pharmacokinetic properties in rat and rhesus, and lead-like physical properties. In a rhesus pharmacodynamic model, compound 19 displays robust, dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels.

SUBMITTER: Hoyt SB 

PROVIDER: S-EPMC4538427 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature