1-芳基-3-烷基-1,4-二氢-4-取代-5H-1,2,4-三唑啉酮-5衍生物的合成及生物活性

被引:3
作者
徐进宜
周宇昕
吴晓明
唐康
王秋娟
机构
[1] 中国药科大学药物化学教研室!南京
[2] 不详
[3] 中国药科大学生理学教研室!南京
关键词
AT1受体拮抗剂; 1-芳基-3-烷基-1,4-二氢-4-取代-5H-1,2,4-三唑啉酮-5; 降压; 合成;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
为寻找新的高效非肽类血管紧张素Ⅱ(AⅡ)受体括抗剂,以SC-51316为先导,运用生物电子等排和拼合原理,设计并合成了9个1-芳基-3-烷基-1,4-二氢-4-取代-5H-1,2,4-三唑啉酮-5衍生物。所有目的化合物均未见文献报道,其结构经IR、1HNMR和MS鉴定。初步体外药理实验表明:在抑制AⅡ诱发的兔主动脉收缩反应模型中,化合物17h具有较好的活性。
引用
收藏
页码:323 / 327
页数:5
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