Article ID Journal Published Year Pages File Type
10594121 Bioorganic & Medicinal Chemistry Letters 2011 6 Pages PDF
Abstract
The selective inhibition of the aspartyl protease renin is of high interest to control hypertension and associated cardiovascular risk factors. Following on preceding contributions, we report herein on the optimization of two series of azaindoles to arrive at potent and non-chiral renin inhibitors. The previously discovered azaindole scaffold was further explored by structure-based drug design in combination with parallel synthesis. This results in the identification of novel 5- or 7-azaindole derivatives with remarkable potency for renin inhibition.
Keywords
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
, , , , , ,