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Design and optimization of renin inhibitors: Orally bioavailable alkyl amines

Authors :
Tice, Colin M.
Xu, Zhenrong
Yuan, Jing
Simpson, Robert D.
Cacatian, Salvacion T.
Flaherty, Patrick T.
Zhao, Wei
Guo, Joan
Ishchenko, Alexey
Singh, Suresh B.
Wu, Zhongren
Scott, Boyd B.
Bukhtiyarov, Yuri
Berbaum, Jennifer
Mason, Jennifer
Panemangalore, Reshma
Cappiello, Maria Grazia
Müller, Dominik
Harrison, Richard K.
McGeehan, Gerard M.
Source :
Bioorganic & Medicinal Chemistry Letters. Jul2009, Vol. 19 Issue 13, p3541-3545. 5p.
Publication Year :
2009

Abstract

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 0.47nM, caused a sustained reduction in mean arterial blood pressure in a double transgenic rat model of hypertension. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
19
Issue :
13
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
41240862
Full Text :
https://doi.org/10.1016/j.bmcl.2009.04.140