Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594121 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
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.
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Authors
Hans Matter, Bodo Scheiper, Henning Steinhagen, Zsolt Böcskei, Valérie Fleury, Gary McCort,