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.
Keywords:
NSAIDs; acetaminophen; analgesic; anti-inflammatory; cyclooxygenase; molecular modeling.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetic Acid
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Analgesics / chemical synthesis
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Analgesics / chemistry
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Analgesics / pharmacology*
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Carrageenan
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Cyclooxygenase 1 / metabolism
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Cyclooxygenase 2 / metabolism
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Cyclooxygenase Inhibitors / chemical synthesis
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / pharmacology*
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Edema / chemically induced
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Edema / drug therapy*
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Edema / metabolism
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Humans
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Ibuprofen / chemical synthesis
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Ibuprofen / chemistry
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Ibuprofen / pharmacology*
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Molecular Structure
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Pain / chemically induced
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Pain / drug therapy*
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Pain / metabolism
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Pain Measurement / drug effects
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Quantitative Structure-Activity Relationship
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Rats
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Stomach Ulcer / drug therapy
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Stomach Ulcer / metabolism
Substances
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Analgesics
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Anti-Inflammatory Agents, Non-Steroidal
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Cyclooxygenase Inhibitors
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Carrageenan
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Cyclooxygenase 1
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Cyclooxygenase 2
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Acetic Acid
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Ibuprofen