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. 2010 Jan 15;20(2):694-9.
doi: 10.1016/j.bmcl.2009.11.066. Epub 2009 Dec 1.

Optimization of orally bioavailable alkyl amine renin inhibitors

Zhenrong Xu  1 , 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
Affiliations

Optimization of orally bioavailable alkyl amine renin inhibitors

Zhenrong Xu et al. Bioorg Med Chem Lett. .

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.

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