Synthesis of some novel oxadiazole and oxadiazoline analogues for their antiinflammatory activity.
The search for newer non-steroidal antiinflammatory drugs (NSAIDs) and the importance of oxadiazoles as antiinflammatory agents prompted us to undertake the synthesis of some novel oxadiazole and related analogues with unreported antiinflammatory activities. The antiinflammatory potential of the compounds was investigated using the carrageenan-induced rat paw edema method and cotton pellet-induced granuloma method. Some compounds demonstrated marked antiinflammatory activities. The antiinflammatory activity of oxadiazoles at doses of 100 mg/kg was shown by their ability to provide 28-55%, 21-36%, and 27-49% protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. On the other hand, the antiinflammatory properties of oxadiazolines at doses of 100 mg/kg was reflected by their ability to provide 15-47%, 22-39%, and 23-47% protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. Structure-activity relationships among synthesized compounds were also studied.
Rajak
Harish
H
SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur-495 009, India. harishdops@yahoo.co.in
Kharya
Murli Dhar
MD
Mishra
Pradeep
P
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005260:Female; D008297:Male; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D010069:Oxadiazoles