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

Authors
SATO M KAWASHIMA Y GOTO J YAMANE Y CHIBA Y JINNO S SATAKE M IMANISHI T IWATA C
Citation
M. Sato et al., SYNTHESIS AND EVALUATION OF NOVEL THIAZOLIDINE DERIVATIVES AS THROMBOXANE-A2 RECEPTOR ANTAGONISTS, Chemical and Pharmaceutical Bulletin, 42(3), 1994, pp. 521-529
Citations number
26
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chemical and Pharmaceutical Bulletin → ACNP
ISSN journal
00092363
Volume
42
Issue
3
Year of publication
1994
Pages
521 - 529
Database
ISI
SICI code
0009-2363(1994)42:3<521:SAEONT>2.0.ZU;2-9
Abstract
A series of 3-benzoyl or 3-phenylsulfonyl-2-substituted thiazolidine d erivatives were synthesized, and evaluated for their thromboxane A2 (T XA2) receptor-antagonizing effect on pha,9alpha-(epoxymethano)prosta-5 (Z),13(E)-dienoic acid (U-46619)-induced aggregation of rabbit platele t-rich plasma (PRP). A simple 2-arylthiazolidine derivative, -benzoyl- 2-(4-hydroxy-3-methoxyphenyl)thiazolidine (5a), showed mild TXA2 recep tor antagonist activity. Modification of 5a led to henylsulfonyl)thiaz olidin-2-ylmethyl]phenoxyacetic acid (29d), which showed 10 times more potent TXA2 receptor antagonist activity than 5a.