1175015-06-1Relevant articles and documents
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
, p. 5480 - 5486 (2011)
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.
CYCLIC AZAINDOLE-3-CARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
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Page/Page column 88-89, (2009/09/05)
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