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 language | English (US) |
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Pages (from-to) | 1369-1386 |
Number of pages | 18 |
Journal | Future Medicinal Chemistry |
Volume | 12 |
Issue number | 15 |
DOIs | |
State | Published - Aug 2020 |
Keywords
- Acetaminophen
- Analgesic
- Anti-inflammatory
- Cyclooxygenase
- Molecular modeling
- Nsaids inflammation is
ASJC Scopus subject areas
- Molecular Medicine
- Pharmacology
- Drug Discovery