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某些5-芳基-2-氨基-1,3,4-恶(硫)二唑的合成与生物学评价

Synthesis and biological evaluation of some 5-aryl-2-amino-1,3,4-oxa(thia)diazoles.

作者信息

Mazzone G, Bonina F, Puglisi G, Arrigo R R, Cosentino C, Blandino G

出版信息

Farmaco Sci. 1982 Oct;37(10):685-700.

PMID:6982830
Abstract

Three series of 5-aryl-2-amino or 2-amino substituted 1,3,4-oxadiazoles (IV-XVIII) were prepared together with the corresponding series of the analogous 5-aryl-2-amino-1,3,4-thiadiazoles (XIX-XXXIII). The purpose of this work is two-fold: to study their pharmacological action in relation to the substituents bound to the positions -2 and -5, and to observe whether the isosteric substitution of the oxygen of he oxadiazolic nucleus with the sulfur leading to a thiadiazolic nucleus causes any activity variation. The AA. report and discuss the results obtained studying the antifungal as well as the antiinflammatory and antipyretic activity of the synthetized compounds.

摘要

制备了三组5-芳基-2-氨基或2-氨基取代的1,3,4-恶二唑(IV-XVIII)以及相应系列的类似5-芳基-2-氨基-1,3,4-噻二唑(XIX-XXXIII)。这项工作有两个目的:研究它们与连接在-2和-5位上的取代基相关的药理作用,以及观察恶二唑核中的氧被硫等排取代形成噻二唑核是否会导致活性变化。作者报告并讨论了研究合成化合物的抗真菌以及抗炎和解热活性所获得的结果。

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