Design, synthesis and biological evaluation of amide derivatives as xanthine oxidase inhibitors
10.16438/j.0513-4870.2017-0251
- VernacularTitle:酰胺类黄嘌呤氧化酶抑制剂的设计合成及活性评价
- Author:
Lei ZHANG
1
;
Ding-an YAN
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, 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;
gout;
amide derivative
- From:
Acta Pharmaceutica Sinica
2017;52(6):952-958
- CountryChina
- Language:Chinese
-
Abstract:
Xanthine oxidase (XO) is a key enzyme in the synthesis of uric acid. Therefore, XO inhibitors play an important role in the antihyperuricemic therapy. Based on the template structures of febuxostat and topiroxostat, 18 amide derivatives were designed and synthesized. Among them, six showed apparent inhibitory activity against XO under the concentration of 10 μmol·L-1. Molecular docking revealed the possible interaction mode of this compound class, which may provide a clue for further molecular design.
