title: Synthesis and Biological Evaluation of Novel Aryl-2H-pyrazole Derivatives as Potent Non-purine Xanthine Oxidase Inhibitors.
abstract: 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.
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University.
authors.forename: Zhi-Gang
authors.initials: ZG
authors.lastname: Sun
authors.forename: Xiao-Jing
authors.initials: XJ
authors.lastname: Zhou
authors.forename: Ming-Li
authors.initials: ML
authors.lastname: Zhu
authors.forename: Wen-Ze
authors.initials: WZ
authors.lastname: Ding
authors.forename: Zhen
authors.initials: Z
authors.lastname: Li
authors.forename: Hai-Liang
authors.initials: HL
authors.lastname: Zhu
mesh_terms: D000818:Animals; D020134:Catalytic Domain / Q000187:drug effects; D002417:Cattle; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D062105:Molecular Docking Simulation; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014969:Xanthine Oxidase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D011720:Pyrazoles; C031280:pyrazole; D014969:Xanthine Oxidase