514182-83-3Relevant academic research and scientific papers
Structure-based optimization of potent 4- and 6-azaindole-3-carboxamides as renin inhibitors
Scheiper, Bodo,Matter, Hans,Steinhagen, Henning,B?cskei, Zsolt,Fleury, Valérie,McCort, Gary
scheme or table, p. 5480 - 5486 (2011/10/09)
The control of hypertension and associated cardiovascular risk factors is possible by selective inhibition of the aspartyl protease renin due to its unique position in the renin-angiotensin system. Starting from a previously disclosed series of potent and nonchiral indole-3-carboxamides, we further explored this motif by structure-based drug design guided by X-ray crystallography in combination with efficient parallel synthesis. This resulted in the discovery of 4- or 6-azaindole derivatives with remarkable potency for renin inhibition. The best compound from these series showed an IC50 value of 1.3 nM.
