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血小板活化因子(PAF)类似物。1. 烷氧基链的一些修饰

Analogues of platelet activating factor (PAF). 1. Some modifications of the alkoxy chain.

作者信息

Wissner A, Sum P E, Schaub R E, Kohler C A, Goldstein B M

出版信息

J Med Chem. 1984 Sep;27(9):1174-81. doi: 10.1021/jm00375a016.

DOI:10.1021/jm00375a016
PMID:6471071
Abstract

Analogues of platelet activating factor (PAF) in which the ether oxygen has been removed (6) and in which the alkoxy chain at C1 has been replaced with a o-, p-, or m-alkylphenoxy group (30, 31, and 35, respectively) have been prepared. Compound 6 shows reduced platelet aggregation and hypotensive activity in comparison with C16 and C18 PAF. The results obtained for compounds 30, 31, and 35 indicate that the hypotensive and platelet aggregating responses are sensitive to structural modification of the ether chain. The ortho analogue 30 shows no platelet aggregating activity and only a weak hypotensive response. The para analogue 31 exhibits a moderate decrease in activity in both assays. The meta analogue 35 is the most active of the three.

摘要

已经制备了血小板活化因子(PAF)的类似物,其中醚氧已被去除(6),并且C1处的烷氧基链已分别被邻、对或间烷基苯氧基取代(分别为30、31和35)。与C16和C18 PAF相比,化合物6显示出降低的血小板聚集和降压活性。化合物30、31和35的结果表明,降压和血小板聚集反应对醚链的结构修饰敏感。邻位类似物30没有血小板聚集活性,只有微弱的降压反应。对位类似物31在两种测定中活性均适度降低。间位类似物35是三者中活性最高的。

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