Cody Wayne L, Holsworth Daniel D, Powell Noel A, Jalaie Mehran, Zhang Erli, Wang Wei, Samas Brian, Bryant John, Ostroski Robert, Ryan Michael J, Edmunds Jeremy J
Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA.
Bioorg Med Chem. 2005 Jan 3;13(1):59-68. doi: 10.1016/j.bmc.2004.09.056.
Recently, trans-disubstituted oxo-aryl-piperidines have been identified as small molecule nonpeptide renin inhibitors for the modulation of hypertension. Herein, we report on the discovery and preparation of a new class of novel cis-disubstituted amino-aryl-piperidines as a mixture of enantiomers that are potent in vitro renin inhibitors and also, possess in vivo antihypertensive activity in a double transgenic mouse model.
最近，反式二取代的氧代芳基哌啶已被鉴定为用于调节高血压的小分子非肽肾素抑制剂。在此，我们报告了一类新型顺式二取代氨基芳基哌啶的发现和制备，其为对映体混合物，是有效的体外肾素抑制剂，并且在双转基因小鼠模型中具有体内抗高血压活性。
