SYNTHESIS AND ACTIVITIES OF NEW ARYLSULFONAMIDO THROMBOXANE-A(2)-RECEPTOR ANTAGONISTS

被引：3

作者：

SARTORI, E ^{[1
]}

CAMY, F ^{[1
]}

TEULON, JM ^{[1
]}

CAUSSADE, F ^{[1
]}

VIRONEODDOS, A ^{[1
]}

CLOAREC, A ^{[1
]}

机构：

[1] UPSA LABS,F-92506 RUEIL MALMAISON,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 28卷 / 7-8期

关键词：

THROMBOXANE-A(2); RECEPTOR ANTAGONIST; PLATELET AGGREGATION; ARYLSULFONAMIDO DERIVATIVE;

D O I：

10.1016/0223-5234(93)90093-T

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New benzoic, benzeneacetic and thiazole-4-acetic acids bearing an arylsulfonamido alkyl or alkylhetero side chain were synthesized and tested in vitro for affinity for human platelet thromboxane A2 receptors and inhibition of U46619-induced rat aortic ring contraction. Influence of substitution patterns, chain length and presence of heteroatoms were studied and compounds within a 30 nmol range for inhibition of U46619-induced contractions were found. One of the most potent, 2-[(4-chloro-benzenesulfonylamino-ethyl)thio] thiazole-4-acetic acid (VII-4) was orally active (1 mg/kg), as evidenced by the inhibition of U46619-induced platelet aggregation in guinea pigs, ex vivo.

引用

页码：625 / 632

页数：8

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