Synthesis of new ibuprofen hybrid conjugates as potential anti-inflammatory and analgesic agents

• Published in: Future medicinal chemistry Vol. 12; no. 15; pp. 1369 - 1386
• Main Authors: Panda, Siva S, Girgis, Adel S, Honkanadavar, Hitesh H, George, Riham F, Srour, Aladdin M
• Format: Journal Article
• Language: English
• Published: England Newlands Press Ltd 01-08-2020
• Subjects: acetaminophen; analgesic; anti-inflammatory; cyclooxygenase; molecular modeling; NSAIDs; anti-inflammatory; cyclooxygenase; acetaminophen; analgesic; molecular modeling; NSAIDs
• ISSN: 1756-8919; 1756-8927
• DOI: 10.4155/fmc-2020-0109

A new set of hybrid conjugates derived from 2-(4-isobutylphenyl)propanoic acid (ibuprofen) is synthesized to overcome the drawbacks of the current non-steroidal anti-inflammatory drugs.
Synthesized conjugates were screened for their anti-inflammatory, analgesic and ulcerogenic properties. Few conjugates were found to have significant anti-inflammatory properties in the carrageenan-induced rat paw edema test, while a fair number of conjugates showed promising peripheral analgesic activity in the acetic acid-induced writhing test as well as central analgesic properties in the
hot plate technique. The newly synthesized conjugates did not display any ulcerogenic liability.
, COX-1 and COX-2 enzyme inhibition studies raveled compound
is more selective toward COX-2 compared with ibuprofen.