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Synthesis and bioactivities of some new 1H-pyrazole derivatives containing an aryl sulfonate moiety

Synthesis and bioactivities of some new 1H-pyrazole derivatives containing an aryl sulfonate moiety

作     者:Babasaheb V.Kendre Mahadev G.Landge Wamanrao N.Jadhav Sudhakar R.Bhusare 

作者机构:Department of ChemistryDnyanopasak College 

出 版 物:《Chinese Chemical Letters》 (中国化学快报(英文版))

年 卷 期:2013年第24卷第4期

页      面:325-328页

核心收录:

学科分类:1007[医学-药学(可授医学、理学学位)] 10[医学] 

主  题:PyrazoleEnaminonep Toluene sulfonyl chlorideAnti inflammatory activityCOX 2 inhibitors 

摘      要:A new series of 1H-pyrazole derivatives 5a-j bearing an aryl sulfonate moiety have been synthesized by a one-pot cyclo-condensation reaction of 2-(3-(dimethylamino)acryloyl)phenyl-4-methyl benzene sulfonates 4a-e and hydrazine hydrate or phenyl hydrazine in ethanol under reflux conditions. Some of the newly synthesized compounds were screened for their anti-inflammatory activity. All synthesized compounds were screened against Gram positive and Gram negative bacterial and fungal strains. The compound 5b was found to be a potent anti-inflammatory agent while the majority of the compounds were found to be active against microbial strains.

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