Synthesis and anti-inflammatory activity of p-(sulfamyl) benzylidene-linked heterocyclic ketone derivatives
10.3321/j.issn:1000-5048.2009.06.004
- VernacularTitle:对氨磺酰基苯亚甲基环酮类化合物的合成及抗炎活性
- Author:
Wenxing HUANG
;
Yisheng LAI
;
Yihua ZHANG
;
Zhenguo WANG
;
Zhihao ZHANG
;
Lin MA
;
Hui JI
- Publication Type:Journal Article
- Keywords:
dual inhibitors of COX and 5-LOX;
heterocyclic ketone derivatives;
anti-inflammatory activity;
gastrointestinal side effects
- From:
Journal of China Pharmaceutical University
2009;40(6):497-502
- CountryChina
- Language:Chinese
-
Abstract:
Aim: To study the synthesis and anti-inflammatory activity of p-(sulfamyl) benzylidene-linked hetero-cyclic ketone derivatives. Methods: A series of p-(sulfamyl) benzylidene-linked heterocyclic ketone derivatives were synthesized. Anti-inflammatory activity was evaluated against xylene-induced ear oedema in mice and against carrageenan-induced paw oedema in rats. Gastrointestinal side effects in the rats were also examined after continu-ous introgastric administration of these compounds once daily for 7 days. Results: Twelve compounds( LHZ-101-LHZ-112) were synthesized and their structures were confirmed by IR, ~1H NMR, MS and elemental analysis. LHZ-105, LHZ-106 and LHZ-111 exhibited marked anti-inflammatory activity in xylene-induced mice ear swelling model. LHZ-106 and LHZ-111 showed significant anti-inflammatory activity in carrageenan-induced rat paw ede-ma model. LHZ-105, LHZ-106 and LHZ-111 had less gastrointestinal side effects than diclofenac sodium and CI-1004. Conclusion: These results suggest that some of these compounds have the potential for anti-inflammatory activity with few gastrointestinal side effects.
