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351.
Asim Raza Dr. Mohsin Abbas Khan Prof. Dr. Irshad Ahmad Dr. Sajid Ur Rehman Dr. Saharish Khaliq Dr. Javed Ahmed Breena Awan Farhat Ullah Anum Masood Naveed Ahmed 《化学与生物多样性》2023,20(7):e202300482
Prodrugs of dexibuprofen having ester moieties instead of free carboxylic acid which involves in gastrointestinal side effects have been synthesized. Dexibuprofen acid was condensed with different alcohols/phenols to afford the ester prodrugs. All of the synthesized prodrugs were characterized by their physical attributes, elemental analysis, FT-IR, 1H-NMR, and 13C-NMR spectroscopy. The in vitro anti-inflammatory studies was done by chemiluminescence technique reflect prodrugs have been more potent, owing to the different chemical structures. Lipoxygenase enzyme inhibition assay was also assess and found compound DR7 with IC50=19.8 μM), DR9 (IC50=24.8 μM) and DR3 (IC50=47.2 μM) as compared with Dexibuprofen (IC50=156.6 μM). It was also evaluated for docking studies revealed that DR7 has found to be more potent anti-inflammatory against 5-LOX (3 V99) as well as analgesic against COX-II (5KIR) enzyme. Anti-oxidant activities were also performed, DR3 (86.9 %), DR5 (83.5 %), DR7 (93.9 %) and DR9 (87.4 %) were found to be more anti-oxidant as compared to (2S)-2-[4-(2-methylpropyl)phenyl]propanoic acid (52.7 %). 相似文献
352.