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4-(4-苯基取代)-1,2,3-三唑乙酸衍生物是前列腺素合成的体外抑制剂。

4-(4-Phenylsubstituted)-1,2,3-triazolacetic acid derivatives in vitro inhibitors of prostaglandin synthesis.

作者信息

Biagi G, Livi O, Da Settimo A, Lucacchini A, Mazzoni M R, Barili P L

出版信息

Farmaco Sci. 1985 Feb;40(2):73-85. doi: 10.1002/chin.198530217.

Abstract

New 4-(4-phenylsubstituted)-1,2,3-triazolacetic acid derivatives of general formula (I) were prepared by nucleophilic substitution, 1,3-dipolar cycloaddition and functional group interconversion reactions. These compounds were evaluated as in vitro prostaglandin synthesis inhibitors. Only the isomeric compounds (II c) and (III e), with a 4-aminophenyl substituent on the triazole ring, inhibit arachidonic acid-induced malondialdehyde formation in human platelets; (II c) and (III e) are as effective as aspirin.

摘要

通过亲核取代、1,3-偶极环加成和官能团相互转化反应制备了通式(I)的新型4-(4-苯基取代)-1,2,3-三唑乙酸衍生物。这些化合物作为体外前列腺素合成抑制剂进行了评估。只有在三唑环上带有4-氨基苯基取代基的异构体化合物(II c)和(III e)能抑制花生四烯酸诱导的人血小板中丙二醛的形成;(II c)和(III e)的效果与阿司匹林相当。

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