Synthesis and biological evaluation of novel aryl-2H-pyrazole derivatives as potent non-purine xanthine oxidase inhibitors
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.
pyrazole xanthine oxidase inhibitory
Zhi-Gang Sun Xiao-Jing Zhou Ming-Li Zhu Wen-Ze Ding Zhen Li Hai-Liang Zh
Stale Key Laboratory of Pharmaceutical Biotechnology,Nanjing University Nanjing 210093,People”s Republic of China
国内会议
大连
英文
783-800
2016-09-24（万方平台首次上网日期，不代表论文的发表时间）