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.