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Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension |
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| Authors: | Scott B Hoyt Jerry Taylor Clare London Amjad Ali Feroze Ujjainwalla Jim Tata Mary Struthers Doris Cully Tom Wisniewski Ning Ren Charlene Bopp Andrea Sok Andreas Verras Daniel McMasters Qing Chen Elaine Tung Wei Tang Gino Salituro Yusheng Xiong |
| Institution: | Merck Research Laboratories, PO Box 2000, NJ 07065, Rahway, United States |
| Abstract: | We report the discovery and hit-to-lead optimization of a structurally novel indazole series of CYP11B2 inhibitors. Benchmark compound 34 from this series displays potent inhibition of CYP11B2, high selectivity versus related steroidal and hepatic CYP targets, and lead-like physical and pharmacokinetic properties. On the basis of these and other data, the indazole series was progressed to lead optimization for further refinement. |
| Keywords: | Aldosterone synthase CYP11B2 Indazole Hit-to-lead Hypertension |
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