Journal
RSC ADVANCES
Volume 6, Issue 115, Pages 114879-114888Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6ra24651f
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Funding
- National Natural Science Foundation of China [81502932, 81673293, 81602969]
- Program for Innovative Research Team of the Ministry of Education
- Program for Liaoning Innovative Research Team in University
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A series of 2-phenyl-5-methyl-2H-1,2,3-triazole-4-carboxylic acids/carbohydrazides as analogues of febuxostat were synthesized and evaluated for their in vitro xanthine oxidase (XO) inhibitory activity. Among these compounds, the carboxylic acid derivatives 7a-h and 8a-h exhibited high potency in the submicromolar/nanomolar range. Steady-state kinetics experiment revealed that 7f was a mixed-type inhibitor of xanthine oxidase. In addition, a molecular docking study of 7f was performed to determine its binding mode at the active site of xanthine oxidase.
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