化学
钾通道
苯并咪唑
立体化学
三唑
结构-活动关系
组合化学
敌手
药理学
体外
受体
生物化学
内科学
有机化学
医学
作者
Heather J. Finlay,Ji Jiang,Yolanda Caringal,Alexander Kover,Mary Lee Conder,Dezhi Xing,Paul Lévesque,Timothy M. Harper,Mei Mann Hsueh,Karnail S. Atwal,Michael A. Blanar,Ruth R. Wexler,John Lloyd
标识
DOI:10.1016/j.bmcl.2013.01.064
摘要
Previously disclosed C6 amido and benzimidazole dihydropyrazolopyrimidines were potent and selective blockers of IKur current. Syntheses and SAR for C6 triazolo and imidazo dihydropyrazolopyrimidines series are described. Trifluoromethylcyclohexyl N(1) triazole, compound 51, was identified as a potent and selective Kv1.5 inhibitor with an acceptable PK and liability profile.
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