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Updated: May 30, 2026

Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Structure-based optimization of potent 4- and 6-azaindole-3-carboxamides as renin inhibitors
Bodo Scheiper1, Hans Matter, Henning Steinhagen
1Sanofi-Aventis, Deutschland GmbH, Chemical and Analytical Sciences, Building G878, D-65926 Frankfurt, Germany.
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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