Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib

被引：56
|
作者：
Feng, Zhiqiang [1 ]
Chu, Fengming [1 ]
Guo, Zongru [1 ]
Sun, Piaoyang [2 ]
机构：
[1] Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China
[2] Hengrui Pharmaceut Co, Lianyungang 222002, Jiangsu, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 08期
关键词：
Imrecoxib; Metabolites; Selective COX-2 inhibitor; CYCLOOXYGENASE-2; INHIBITOR; ROFECOXIB; SYNTHASE; RAT;
D O I：
10.1016/j.bmcl.2009.02.090
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We have developed a novel and moderately selective COX-2 inhibitor, imrecoxib, as a new anti-inflammatory drug. We describe herein the preparation of the major metabolites M2 and M4 of imrecoxib, as well as the in vitro and in vivo activities of the two compounds. The results showed that both M2 and M4 are potential COXs inhibitors with a moderate COX-1/COX-2 selectivity, and their anti-inflammatory activity in vivo was equal to or slightly higher than the clinical celecoxib. (c) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2270 / 2272
页数：3
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