Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib.
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.
Feng
Zhiqiang
Z
Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing, China.
Chu
Fengming
F
Guo
Zongru
Z
Sun
Piaoyang
P
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000378:metabolism* / Q000627:therapeutic use; D000068579:Celecoxib; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000188:drug therapy / Q000378:metabolism; D006801:Humans; D051379:Mice; D011720:Pyrazoles / Q000737:chemistry; D011758:Pyrroles / Q000138:chemical synthesis* / Q000378:metabolism* / Q000627:therapeutic use; D051381:Rats; D013440:Sulfides / Q000138:chemical synthesis* / Q000378:metabolism* / Q000627:therapeutic use; D013449:Sulfonamides / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; C488833:Imrecoxib; D011720:Pyrazoles; D011758:Pyrroles; D013440:Sulfides; D013449:Sulfonamides; D000068579:Celecoxib