| Literature DB >> 28416132 |
Scott B Hoyt1, Jerry Taylor2, Clare London2, Amjad Ali2, Feroze Ujjainwalla2, Jim Tata2, Mary Struthers2, Doris Cully2, Tom Wisniewski2, Ning Ren2, Charlene Bopp2, Andrea Sok2, Andreas Verras2, Daniel McMasters2, Qing Chen2, Elaine Tung2, Wei Tang2, Gino Salituro2, Joe Clemas2, Gaochao Zhou2, Douglas MacNeil2, Ruth Duffy2, Yusheng Xiong2.
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.Entities:
Keywords: Aldosterone synthase; CYP11B2; Hit-to-lead; Hypertension; Indazole
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Year: 2017 PMID： 28416132 DOI： 10.1016/j.bmcl.2017.04.021
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823