Design, synthesis and biological evaluation of oxadiazole derivatives as xanthine oxidase inhibitors

Xanthine oxidase (XO) is an important target for the treatment of hyperuricemia and gout. Based on the two known non-purine xanthine oxidase inhibitors, febuxostat and topiroxostat, 14 oxadiazole derivatives have been designed and synthesized. These compounds have been evaluated against XO and five...

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Veröffentlicht in:	Yao hsüeh hsüeh pao 2016-06, Vol.51 (6), p.954-960
Hauptverfasser:	Yan, Ding-an, Zhang, Lei, Tian, Jin-ying, Ye, Fei, Xiao, Zhi-yan
Format:	Artikel
Sprache:	chi
Schlagworte:	Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Febuxostat Gout Gout Suppressants - chemical synthesis Gout Suppressants - pharmacology Humans Hyperuricemia Oxadiazoles - pharmacology Xanthine Oxidase - antagonists & inhibitors
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Zusammenfassung:	Xanthine oxidase (XO) is an important target for the treatment of hyperuricemia and gout. Based on the two known non-purine xanthine oxidase inhibitors, febuxostat and topiroxostat, 14 oxadiazole derivatives have been designed and synthesized. These compounds have been evaluated against XO and five of them exhibited significant inhibitory activities at the concentrations below 10 μmol·L(-1).
ISSN:	0513-4870
DOI:	10.16438/j.0513-4870.2016-0278