- Structure-based design and optimization of potent renin inhibitors on 5- or 7-azaindole-scaffolds
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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. The best compounds on both series show IC50 values between 3 and 8 nM.
- Matter, Hans,Scheiper, Bodo,Steinhagen, Henning,B?cskei, Zsolt,Fleury, Valérie,McCort, Gary
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scheme or table
p. 5487 - 5492
(2011/10/12)
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- CYCLIC AZAINDOLE-3-CARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
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The present invention relates to cyclic azaindole-3-carboxamides of the formula (I) wherein A, R, R10, R20, R30, R40, Y1, Y2, Y3, Y4, n, p and q have the meanings indi
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Page/Page column 121
(2009/09/05)
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