Design, synthesis and biological evaluation of oxadiazole derivatives as xanthine oxidase inhibitors
10.16438/j.0513-4870.2016-0278
- VernacularTitle:噁二唑类黄嘌呤氧化酶抑制剂的设计合成及活性评价
- Author:
Ding-an YAN
1
;
Lei ZHANG
1
;
Jin-ying TIAN
2
;
Fei YE
2
;
Zhi-yan XIAO
1
Author Information
1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
2. Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
xanthine oxidase;
hyperuricemia;
oxadiazole derivative
- From:
Acta Pharmaceutica Sinica
2016;51(6):954-
- CountryChina
- Language:Chinese
-
Abstract:
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.
