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血小板激活因子(PAF)类似物。2.甘油主链的一些修饰

Analogues of platelet activating factor (PAF). 2. Some modifications of the glycerine backbone.

作者信息

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

出版信息

J Med Chem. 1985 Sep;28(9):1181-7. doi: 10.1021/jm00147a010.

Abstract

Racemic analogues of platelet activating factor (PAF) that contain a methylene group between the C2 and C3 carbon atoms (39) or between the C1 and C2 carbon atoms (40) have been synthesized. These compounds show reduced platelet aggregation and hypotensive activity as measured against racemic C16 PAF. Compounds in which the C1 carbon atom of PAF is substituted with one or two methyl groups (41 and 42, respectively) or the C3 carbon is substituted with a single methyl group (43) have been synthesized. Platelet aggregation and hypotensive responses produced by these compounds are significantly less than those obtained with racemic C16 PAF. None of the above compounds exhibit a separation of the platelet aggregation and hypotensive activities.

摘要

已合成了血小板活化因子(PAF)的外消旋类似物,这些类似物在C2和C3碳原子之间(39)或C1和C2碳原子之间(40)含有一个亚甲基。相对于外消旋C16 PAF,这些化合物显示出降低的血小板聚集和降压活性。已合成了其中PAF的C1碳原子被一个或两个甲基取代(分别为41和42)或C3碳原子被单个甲基取代(43)的化合物。这些化合物产生的血小板聚集和降压反应明显小于外消旋C16 PAF产生的反应。上述化合物均未表现出血小板聚集和降压活性的分离。

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