Chemical and Pharmaceutical Bulletin p. 521 - 529 (1994)
Update date:2022-08-02
Topics:
Sato
Kawashima
Goto
Yamane
Chiba
Jinno
Satake
Imanishi
Iwata
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-11α,9α- (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]phenoxyaretic acid (29d), which showed 10 times more potent TXA2 receptor antagonist activity than 5a.
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