二氟尼柳衍生物的研究进展

Advance on Study of Diflunisal Derivatives

综述了以二氟尼柳为先导化合物,通过成盐、O-酰基化、酯化和酰胺化等反应,进行结构修饰,得到一系列衍生物。经药理活性研究显示,部分衍生物具有更强的抗炎、镇痛及退热效果、较小的副作用等优点。特别是特殊基团的引入,有可能使其具有抗肿瘤等活性,这将为今后二氟尼柳的结构修饰与活性研究产生较大的促进作用。

This article summarizes the structure modification of Diflunisal through salification, O-acylation, esterification or amidation and activity studies of its derivatives. Diflunisal derivatives exhibit stronger antiinflammatory, antipyretic and analgesic effects with lower gastric toxicity. Especially, when specific groups are introduced, they may have anti-tumor and other activities, which will accelerate the further research of the synthesis and activity studies of new derivatives.