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

…, M Jalaie, E Zhang, W Wang, B Samas, J Bryant…

Index: 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. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 1 p. 59 - 68

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Citation Number: 27

Abstract

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.