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Bioorg Med Chem Lett. 2010 Nov 1;20(21):6286-90. doi: 10.1016/j.bmcl.2010.08.086. Epub 2010 Aug 22.

Design and optimization of new piperidines as renin inhibitors.

Author information

1
Drug Discovery Chemistry & Biochemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland.

Abstract

The discovery of a new series of piperidine-based renin inhibitors is described herein. SAR optimization upon the P3 renin sub-pocket is described, leading to the discovery of 9 and 41, two bioavailable renin inhibitors orally active at low doses in a transgenic rat model of hypertension.

PMID:
20843686
DOI:
10.1016/j.bmcl.2010.08.086
[Indexed for MEDLINE]

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