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Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-inflammatory agents
Authors:Guang-Xiang Zhong  Jin-Qing Hu  Kun Zhao  Lu-Lu Chen  Wei-Xiao Hu  Ming-You Qiu
Institution:College of Pharmaceutical Science, Zhejiang University of Technology, 18, Chaowang Road, Hangzhou, Zhejiang 310032, China
Abstract:To improve the medicinal activity, the structure of diflunisal has been modified. Twenty-one amide derivatives of diflunisal were synthesized starting from diflunisal in three steps with total yields from 72% to 89%. All compounds were identified by 1H NMR, MS, and elemental analysis. The anti-inflammatory and analgesic activities for 19 compounds were evaluated. It was found that 5m possesses an excellent anti-inflammatory activity and a good analgesic activity, maybe a potential anti-inflammatory agent.
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