| Literature DB >> 19959358 |
Zhenrong Xu1, Salvacion Cacatian, Jing Yuan, Robert D Simpson, Lanqi Jia, Wei Zhao, Colin M Tice, Patrick T Flaherty, Joan Guo, Alexey Ishchenko, Suresh B Singh, Zhongren Wu, Brian M McKeever, Boyd B Scott, Yuri Bukhtiyarov, Jennifer Berbaum, Jennifer Mason, Reshma Panemangalore, Maria Grazia Cappiello, Ross Bentley, Christopher P Doe, Richard K Harrison, Gerard M McGeehan, Lawrence W Dillard, John J Baldwin, David A Claremon.
Abstract
Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC(50) of 0.83nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10mg/kg resulted in >20h reduction of blood pressure in a double transgenic rat model of hypertension. Copyright 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 19959358 DOI： 10.1016/j.bmcl.2009.11.066
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823