Synthesis of new 3,4-disubstituted pyrrolidines as thromboxane A(2) prostaglandin H-2 (TP) receptor antagonists

被引:33
作者
Dubuffet, T [1 ]
Muller, O [1 ]
Simonet, SS [1 ]
Descombes, JJ [1 ]
Laubie, M [1 ]
Verbeuren, TJ [1 ]
Lavielle, G [1 ]
机构
[1] INST RECH SERVIER,F-92150 SURESNES,FRANCE
关键词
D O I
10.1016/0960-894X(96)00021-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and TP-receptor antagonistic activity of a series of 3,4-disubstituted pyrrolidines is described. The sulfonamide 1h was the most potent TP-receptor antagonist in this series with a pA(2) value of 9.5 in isolated guinea pig trachea.
引用
收藏
页码:349 / 352
页数:4
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