SYNTHESIS AND EVALUATION OF NOVEL THIAZOLIDINE DERIVATIVES AS THROMBOXANE-A2 RECEPTOR ANTAGONISTS

被引：0
|
作者：
SATO, M
KAWASHIMA, Y
GOTO, J
YAMANE, Y
CHIBA, Y
JINNO, S
SATAKE, M
IMANISHI, T
IWATA, C
机构：
[1] NIPPON SUISAN KAISHA LTD, CENT RES LAB, HACHIOJI, TOKYO 192, JAPAN
[2] OSAKA UNIV, FAC PHARMACEUT SCI, SUITA, OSAKA 565, JAPAN
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1994年 / 42卷 / 03期
关键词：
THROMBOXANE-A2; TXA2; RECEPTOR; ANTAGONIST; THIAZOLIDINE; STRUCTURE ACTIVITY RELATIONSHIP;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 3-benzoyl or 3-phenylsulfonyl-2-substituted thiazolidine derivatives were synthesized, and evaluated for their thromboxane A2 (TXA2) receptor-antagonizing effect on (15S)-15-hydroxy-11alpha,9alpha-(epoxymethano)prosta-5(Z),13(E)-dienoic acid (U-46619)-induced aggregation of rabbit platelet-rich plasma (PRP). A simple 2-arylthiazolidine derivative, 3-benzoyl-2-(4-hydroxy-3-methoxyphenyl)thiazolidine (5a), showed mild TXA2 receptor antagonist activity. Modification of 5a led to 2-chloro-4-[3-(4-chlorophenylsulfonyl)thiazolidin-2-ylmethyl]phenoxyacetic acid (29d), which showed 10 times more potent TXA2 receptor antagonist activity than 5a.
引用
收藏
页码：521 / 529
页数：9
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