| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375380 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
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 resulted in >20 h reduction of blood pressure in a double transgenic rat model of hypertension.
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Authors
Zhenrong Xu, 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,