Synthesis and xanthine oxidase inhibitory activities of 2-phenyl-tetrahydrothiopyrano［4, 3-d］ pyrimidine derivatives
10.11665/j.issn.1000-5048.20150306
- VernacularTitle:2-苯基-四氢噻喃并嘧啶类化合物的合成及黄嘌呤氧化酶抑制活性
- Author:
Jing LI
1
;
Yuejiao REN
;
Su GUAN
;
Lei ZHANG
Author Information
1. 华南理工大学生物科学与工程学院
- Publication Type:Journal Article
- Keywords:
tetrahydrothiopyran;
pyrimidine;
synthesis;
xanthine oxidase inhibitor;
inhibitory activities
- From:
Journal of China Pharmaceutical University
2015;46(3):294-300
- CountryChina
- Language:Chinese
-
Abstract:
Twelve novel 2-phenyl -tetrahydrothiopyrano［4, 3-d］pyrimidine derivatives were synthesized from 4-hydroxy-benzonitrile by etherification, hydrolysis, acylation and addition reactions, etc. The inhibitory activities against xanthine oxidase were evaluated in vitro. Results showed that compounds 8a-8h exhibited varying inhibitory potencies on xanthine oxidase at 100 μmol/L, significantly better than those of compounds 6a-6d, indicating that carboxy-substituted pyrimidine is beneficial to the inhibitory activity. Among compounds 8a-8h, 8f with isopropionic acid-substituted pyrimidine and ethyl-substituted phenol showed the best inhibition with IC50 of 76. 0 μmol/L.
