Design, synthesis and evaluation of oxadiazoles as novel XO inhibitors
10.16438/j.0513-4870.2024-0820
- VernacularTitle:噁二唑类化合物的设计、合成及黄嘌呤氧化酶抑制活性研究
- Author:
Hong-zhan WANG
1
,
2
;
Ya-jun YANG
3
;
Ying YANG
3
;
Fei YE
4
;
Jin-ying TIAN
4
;
Chuan-ming ZHANG
1
;
Zhi-yan XIAO
3
Author Information
1. School of Pharmacy, Baotou Medical College, Inner Mongolia University of Science and Technology, Baotou
2. 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
3. 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
4. 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
- Publication Type:Research Article
- Keywords:
xanthine oxidase;
xanthine oxidase inhibitor;
oxadiazole;
hyperuricemia;
gout
- From:
Acta Pharmaceutica Sinica
2025;60(1):164-171
- CountryChina
- Language:Chinese
-
Abstract:
Xanthine oxidase (XO) is an important therapeutic target for the treatment of hyperuricemia and gout. Based on the previously identified potent XO inhibitor 1, seventeen oxadiazoles and their ring-opening analogues were designed and synthesized via the bioisostere replacement strategy. Among them, compounds 2l, 2n, and 3b showed obvious XO inhibitory activity at the concentration of 10 μmol·L-1, and compound 3b exhibited an IC50 value of 1.45 μmol·L-1.
