Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Scott B Hoyt,Whitney Petrilli,Clare London,Gui-Bai Liang,Jim Tata,Qingzhong Hu,Lina Yin,Chris J van Koppen,Rolf W Hartmann,Mary Struthers,Tom Wisniewski,Ning Ren, Charlene Bopp, Andrea Sok,Tian-Quan Cai,Sloan Stribling,Lee-Yuh Pai,Xiuying Ma,Joe Metzger,Andreas Verras,Daniel McMasters,Qing Chen,Elaine Tung,Wei Tang,Gino Salituro,Nicole Buist, Joe Clemas,Gaochao Zhou,Jack Gibson, Carrie Ann Maxwell, Mike Lassman, Theresa McLaughlin,Jose Castro-Perez,Daphne Szeto,Gail Forrest,Richard Hajdu, Mark Rosenbach,Yusheng Xiong

ACS medicinal chemistry letters（2015）

引用 16|浏览39

暂无评分

摘要

Hit-to-lead efforts resulted in the discovery of compound 19, a potent CYP11B2 inhibitor that displays high selectivity vs related CYPs, good pharmacokinetic properties in rat and rhesus, and lead-like physical properties. In a rhesus pharmacodynamic model, compound 19 displays robust, dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels.

查看译文

AI 理解论文

溯源树

样例

生成溯源树，研究论文发展脉络

Chat Paper

正在生成论文摘要