Synthesis and evaluation of novel thiazolidine derivatives as thromboxane A2 receptor antagonists

DOI: 10.1248/cpb.42.521

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 521 - 529 (1994)

Update date:2022-08-02

Topics:

Authors:

Sato Sato

Kawashima

Goto Goto

Yamane Yamane

Chiba Chiba

Jinno Jinno

Satake Satake

Imanishi

Iwata Iwata

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Article abstract of DOI:10.1248/cpb.42.521

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.

Full text of DOI:10.1248/cpb.42.521

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