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  • Title: 2-(3-Pyridyl)thiazolidine-4-carboxamides. 1. Novel orally active antagonists of platelet-activating factor (PAF).
    Author: Nagaoka H, Hara H, Suzuki T, Takahashi T, Takeuchi M, Matsuhisa A, Saito M, Yamada T, Tomioka K, Mase T.
    Journal: Chem Pharm Bull (Tokyo); 1997 Oct; 45(10):1659-64. PubMed ID: 9353894.
    Abstract:
    In a search for novel platelet-activating factor (PAF) antagonists, we found that 1-(3-phenylpropyl)-4-[2-(3-pyridyl)thiazolidine-4-carbonyl] piperazine (3x) showed in vitro and in vivo PAF-antagonistic activities. Introduction of functional groups at the benzylic methylene carbon of 3x afforded some compounds with more potent PAF-antagonistic activity than 3x. Among them 1-(3-methyl-3-phenylbutyl)-4-[2-(3-pyridyl) thiazolidine-4-carbonyl]-piperazine fumarate (3al, YM264) was found to be one of the most potent PAF antagonists.
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