884510-87-6Relevant articles and documents
Optimization of orally bioavailable alkyl amine renin inhibitors
Xu, Zhenrong,Cacatian, Salvacion,Yuan, Jing,Simpson, Robert D.,Jia, Lanqi,Zhao, Wei,Tice, Colin M.,Flaherty, Patrick T.,Guo, Joan,Ishchenko, Alexey,Singh, Suresh B.,Wu, Zhongren,McKeever, Brian M.,Scott, Boyd B.,Bukhtiyarov, Yuri,Berbaum, Jennifer,Mason, Jennifer,Panemangalore, Reshma,Cappiello, Maria Grazia,Bentley, Ross,Doe, Christopher P.,Harrison, Richard K.,McGeehan, Gerard M.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
scheme or table, p. 694 - 699 (2010/06/16)
Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC50 of 0.83 nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10 mg/kg
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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Page/Page column 82-83, (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
