摘要
吡咯烷衍生物与环氧环戊烷开环反应后,与3,4-二甲氧基苯乙氧基中间体对接,再经钯碳加氢脱保护得维纳卡兰类似物,并通过全细胞膜片钳技术,探讨其对Kv 1.5钾通道电流的阻断效果。结果显示,类似物1a、1b和1c抑制Kv1.5钾通道的IC50分别为sustain current:37,77,30;peak current:89,389,157(μM),且呈浓度和时间依赖性。
The Vernakalant analogues were synthesized through a series reactions including using pyrrolidine derivatives reaction with epoxy cyclopentane by ring-opening reaction, coupling reaction with 3,4- dimethoxyphenethyl alcohol intermediate, and followed by deprotection reaction by Pd/C-H2. The blockade activity against Kv1.5 potassium channel were evaluated using the whole-cell patch clamp technique. The results showeda significant dose and time dependent block on Kv 1.5 potassium channel. The IC50 of analogues 1a, 1b and lc of sustain current were37, 77,and 30, respectively; peak current were 89, 389, and 157 （μM） respectively.
出处
《精细化工中间体》
CAS
2015年第4期31-35,共5页
Fine Chemical Intermediates
基金
2015年度台州职业技术学院校级重点课题(2015ZD08)资助
