1 research outputs found
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys
Hit-to-lead
efforts resulted in the discovery of compound <b>19</b>, 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 <b>19</b> displays robust, dose-dependent aldosterone
lowering efficacy, with no apparent effect on cortisol levels