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Bioorg Med Chem Lett. 2011 Jul 1;21(13):3976-81. doi: 10.1016/j.bmcl.2011.05.014. Epub 2011 May 14.

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.

Author information

1
Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Québec, Canada H9H 3L1. austin.chihyu.chen@gmail.com

Abstract

The design and optimization of a novel series of renin inhibitor is described herein. Strategically, by committing the necessary resources to the development of synthetic sequences and scaffolds that were most amenable for late stage structural diversification, even as the focus of the SAR campaign moved from one end of the molecule to another, highly potent renin inhibitors could be rapidly identified and profiled.

PMID:
21641209
DOI:
10.1016/j.bmcl.2011.05.014
[Indexed for MEDLINE]

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