An Overview on Ibuprofen Derivatives: Advancements in NSAIDs for Enhanced Anti-inflammatory and Analgesic Efficacy

Non-steroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen, are widely used for pain relief and inflammation management. However, their clinical utility is often limited by gastrointestinal side effects arising from non-selective inhibition of both COX-1 and COX-2 enzymes. To address this issue, the ibuprofen derivatives with structural modifications aimed at enhancing COX-2 selectivity while minimizing COX-1 inhibition. The approach involved incorporating specific functional groups and substituents into the ibuprofen scaffold to modulate its binding affinity and selectivity for the COX-2 active site. These modifications were guided by computational modeling, molecular docking and structure-activity relationship (SAR) studies. The synthesis of the novel ibuprofen derivative such as ibuprofen amide and ibuprofen acyl hydrazide derivatives, ibuprofen quinoline conjugate, ibuprofen with hydroxyl group or hetero atoms has been investigate with the help of computational technology. The cucumis melo is also reported to posses anti-ulcer potential and study investigated the mechanism of underlying the anti-ulcer potential. All the molecule showed higher affinity towards Cox-2 enzyme as compared to traditional ibuprofen and also have cucumis melo showed ability to mitigate ulcer and posses anti- ulcer effect.