Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5- oxopiperazin-1-yl]piperidine-3-carboxamides as potent renin inhibitors

摘要

Utilizing X-ray crystal structure analysis, (3S,5R)-5-[4-(2-chlorophenyl)- 2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides were designed and identified as renin inhibitors. The most potent compound 15 demonstrated favorable pharmacokinetic and pharmacodynamic profiles in rat.