化学
钾通道
吡那地尔
钾
钾通道开放器
克罗马卡林
敌手
药理学
离子通道
作者
Heather Finlay,Ji Jiang,Yolanda Caringal,Alexander Kover,Mary Lee Conder,Dezhi Xing,Paul Levesque,Timothy W. 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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