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The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors

2004; Elsevier BV; Volume: 13; Issue: 1 Linguagem: Inglês

10.1016/j.bmc.2004.09.056

1464-3391

Wayne L. Cody, Daniel D. Holsworth, Noel A. Powell, Mehran Jalaie, Erli Zhang, Wei Wang, Brian Samas, John W. Bryant, Robert Ostroski, Michael J. Ryan, Jeremy J. Edmunds,

Receptor Mechanisms and Signaling

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.