Literature DB >> 20843686

Design and optimization of new piperidines as renin inhibitors.

Olivier Corminboeuf1, Olivier Bezençon, Corinna Grisostomi, Luboš Remeň, Sylvia Richard-Bildstein, Daniel Bur, Lars Prade, Patrick Hess, Panja Strickner, Walter Fischli, Beat Steiner, Alexander Treiber.   

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.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20843686     DOI: 10.1016/j.bmcl.2010.08.086

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Investigation of combined CYP3A4 inductive/inhibitory properties by studying statin interactions: a model study with the renin inhibitor ACT-178882.

Authors:  Jasper Dingemanse; Laurent B Nicolas; Luc van Bortel
Journal:  Eur J Clin Pharmacol       Date:  2014-04-15       Impact factor: 2.953

2.  Exploring the substructural space of indole-3-carboxamide derivatives binding to renin: a novel active-site spatial partitioning approach.

Authors:  Tao Jing; Jian Feng; Yumei Zuo; Boli Ran; Jianping Liu; Guoxiang He
Journal:  J Mol Model       Date:  2012-05-16       Impact factor: 1.810

3.  Significant reduction in errors associated with nonbonded contacts in protein crystal structures: automated all-atom refinement with PrimeX.

Authors:  Jeffrey A Bell; Kenneth L Ho; Ramy Farid
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2012-07-17
  3 in total

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