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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

2012; Elsevier BV; Volume: 22; Issue: 24 Linguagem: Inglês

10.1016/j.bmcl.2012.09.103

1464-3405

Yutaka Mori, Yasuyuki Ogawa, Akiyoshi Mochizuki, Yuji Nakamura, Chie Sugita, Shojiro Miyazaki, Kazuhiko Tamaki, Yumi Matsui, Mizuki Takahashi, Takahiro Nagayama, Yoko Nagai, Shinichi Inoue, Takahide Nishi,

Nitric Oxide and Endothelin Effects

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.