Synthetic Strategies for the Development of Ibuprofen Derivatives: A Classified Study

Ibuprofen, a widely used NSAID from the aryl propionic acid class, effectively relieves pain, fever, and inflammation. On prolonged use, it leads to gastrointestinal, hepatic, and renal toxicities, particularly gastrointestinal ulcers. These side effects are largely attributed to the carboxylic acid functional group common to NSAIDs. The present review highlights the different modifications done to the carboxylic group in Ibuprofen, by various researchers such as esters, amides, hydroxamic acids, and N-substituted hydrazides, along with the integration of heterocyclic moieties like triazoles, tetrazoles, and oxadiazoles. Additionally, Ibuprofen has been hybridized with other drugs and complexed with metals to enhance therapeutic effects. The different synthetic strategies that were employed were esterification, amidation, condensation, Schiff’s base formation, etc. These modifications have resulted in derivatives with antimicrobial, antifungal, anticancer, and other biological activities, aiming to reduce side effects while retaining or enhancing anti-inflammatory, analgesic, and antipyretic properties.