Pharmacological evaluation and preparation of nonsteroidal anti-inflammatory drugs containing an N-acyl hydrazone subunit.

摘要: A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies performed that suggest compounds 4a–e bind to cyclooxygenase (COX)-1 COX-2 isoforms, but with higher affinity for COX-2. The display similar activities in vivo, although compound 4c is the most effective inhibiting rat paw edema, a reduction extent inflammation 35.9% 52.8% at 2 4 h, respectively. activity was inferior their respective parent drugs, except after 5 h. Ulcerogenic revealed are less gastrotoxic than drug. Compounds 4b–e demonstrated mucosal damage comparable celecoxib. vivo analgesic drug 4a–b 4d–e. Compound 4a more active dipyrone reducing acetic-acid-induced abdominal constrictions. Our results indicate reduced gastrotoxicity compared non-steroidal drugs.