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Design and optimization of renin inhibitors: Orally bioavailable alkyl amines |
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| Authors: | Colin M. Tice Zhenrong Xu Jing Yuan Robert D. Simpson Salvacion T. Cacatian Patrick T. Flaherty Wei Zhao Joan Guo Alexey Ishchenko Suresh B. Singh Zhongren Wu Boyd B. Scott Yuri Bukhtiyarov Jennifer Berbaum Jennifer Mason Reshma Panemangalore Maria Grazia Cappiello Dominik Müller Richard K. Harrison Gerard M. McGeehan David A. Claremon |
| Affiliation: | 1. Vitae Pharmaceuticals, 502 West Office Center Drive, Fort Washington, PA 19034, USA;2. Charité Berlin, Dept of Pediatric Nephrology, Augustenburger Platz 1, 13353 Berlin, Germany |
| Abstract: | Structure-based drug design led to the identification of a novel class of potent, low MW alkylamine renin inhibitors. Oral administration of lead compound 21l, with MW of 508 and IC50 of 0.47 nM, caused a sustained reduction in mean arterial blood pressure in a double transgenic rat model of hypertension. |
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