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  5. Synthesis and biological evaluation of novel aryl-2H-pyrazole derivatives as potent non-purine xanth

Synthesis and biological evaluation of novel aryl-2H-pyrazole derivatives as potent non-purine xanth

来源 :第八届国际分子模拟与信息技术应用学术会议 | 被引量 : 0次 | 上传用户：zwj_10061
【摘 要】
：
A series of aryl-2H-pyrazole derivatives were synthesized and evaluated for inhibitory activity against xanthine oxidase in vitro as potent xanthine oxidase inhibitors.Among them,2 aryl-2H-pyrazole de
【作 者】
：
Zhi-Gang Sun Xiao-Jing Zhou Ming-Li Zhu Wen-Ze Ding Zhen Li Hai-Liang Zh 
【机 构】
：
Stale Key Laboratory of Pharmaceutical Biotechnology,Nanjing University Nanjing 210093,People's Rep
【出 处】
：
第八届国际分子模拟与信息技术应用学术会议
【发表日期】
：
2016年4期
【关键词】
：
pyrazole xanthine oxidase inhibitory 
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　　A series of aryl-2H-pyrazole derivatives were synthesized and evaluated for inhibitory activity against xanthine oxidase in vitro as potent xanthine oxidase inhibitors.Among them,2 aryl-2H-pyrazole derivatives showed significant inhibitory activities against xanthine oxidase.Compound 19 emerged as the most potent xanthine oxidase inhibitor(IC50=9.8 μM)in comparison with allopurinol(IC50= 9,5 μM).The docking study revealed that compound 19 might have strong interactions with the active site of xanthine oxidase.This compound is thus a new candidate for further development for the treatment of gout.
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