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

Siva S. Panda, Adel S. Girgis, Hitesh H. Honkanadavar, Riham F. George, Aladdin M. Srour

Research output: Contribution to journalArticle

Abstract

Background: 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. Results & methodology: 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 in vivo hot plate technique. The newly synthesized conjugates did not display any ulcerogenic liability. Conclusion:In vitro, COX-1 and COX-2 enzyme inhibition studies raveled compound 7e is more selective toward COX-2 compared with ibuprofen.

Original languageEnglish (US)
Pages (from-to)1369-1386
Number of pages18
JournalFuture Medicinal Chemistry
Volume12
Issue number15
DOIs
StatePublished - Aug 1 2020

Keywords

  • acetaminophen
  • analgesic
  • anti-inflammatory
  • cyclooxygenase
  • molecular modeling
  • NSAIDs

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

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