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  • Title: Structure-based optimization of potent 4- and 6-azaindole-3-carboxamides as renin inhibitors.
    Author: Scheiper B, Matter H, Steinhagen H, Böcskei Z, Fleury V, McCort G.
    Journal: Bioorg Med Chem Lett; 2011 Sep 15; 21(18):5480-6. PubMed ID: 21840218.
    Abstract:
    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 IC(50) value of 1.3 nM.
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