1438393-11-3Relevant articles and documents
Discovery of VTP-27999, an alkyl amine renin inhibitor with potential for clinical utility
Jia, Lanqi,Simpson, Robert D.,Yuan, Jing,Xu, Zhenrong,Zhao, Wei,Cacatian, Salvacion,Tice, Colin M.,Guo, Joan,Ishchenko, Alexey,Singh, Suresh B.,Wu, Zhongren,McKeever, Brian M.,Bukhtiyarov, Yuri,Johnson, Judith A.,Doe, Christopher P.,Harrison, Richard K.,McGeehan, Gerard M.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
, p. 747 - 751 (2011/12/01)
Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the cyclohexylmethyl group occupying the S1 pocket with a (R)-(tetrahydropyran-3-yl)
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines
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,Mueller, Dominik,Harrison, Richard K.,McGeehan, Gerard M.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
scheme or table, p. 3541 - 3545 (2010/03/31)
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 bl
DIAMINOPROPANOL RENIN INHIBITORS
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, (2008/06/13)
Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease me
