1174926-85-2Relevant academic research and scientific papers
Discovery and optimization of a new class of potent and non-chiral indole-3-carboxamide-based renin inhibitors
Scheiper, Bodo,Matter, Hans,Steinhagen, Henning,Stilz, Ulrich,B?cskei, Zsolt,Fleury, Valérie,McCort, Gary
scheme or table, p. 6268 - 6272 (2010/11/18)
Selective inhibition of the aspartyl protease renin has gained attraction as an interesting approach to control hypertension and associated cardiovascular risk factors given its unique position in the renin-angiotensin system. Using a combination of high-throughput screening, parallel synthesis, X-ray crystallography and structure-based design, we identified and optimized a novel series of potent and non-chiral indole-3-carboxamides with remarkable potency for renin. The most potent compound 5k displays an IC50 value of 2 nM.
