2-(3-PYRIDYL)THIAZOLIDINE-4-CARBOXAMIDES .1. NOVEL ORALLY-ACTIVE ANTAGONISTS OF PLATELET-ACTIVATING-FACTOR (PAF)

Authors
NAGAOKA H HARA H SUZUKI T TAKAHASHI T TAKEUCHI M MATSUHISA A SAITO M YAMADA T TOMIOKA K MASE T
Citation
H. Nagaoka et al., 2-(3-PYRIDYL)THIAZOLIDINE-4-CARBOXAMIDES .1. NOVEL ORALLY-ACTIVE ANTAGONISTS OF PLATELET-ACTIVATING-FACTOR (PAF), Chemical and Pharmaceutical Bulletin, 45(10), 1997, pp. 1659-1664
Citations number
23
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chemical and Pharmaceutical Bulletin → ACNP
ISSN journal
00092363
Volume
45
Issue
10
Year of publication
1997
Pages
1659 - 1664
Database
ISI
SICI code
0009-2363(1997)45:10<1659:2.NOA>2.0.ZU;2-3
Abstract
In a search for novel platelet-activating factor (PAF) antagonists, we found that 4-[2-(3-pyridyl)thiazolidine-4-carbonyl]piperazine (3x) sh owed in vitro and in vivo PAF-antagonistic activities, Introduction of functional groups at the benzylic methylene carbon of 3x afforded som e compounds with more potent PAF-antagonistic activity than 3x. Among them 4-[2-(3-pyridyl)thiazolidine-4-carbonyl]piperazine fumarate (3al, YM264) was found to be one of the most potent PAF antagonists.