Tailored [1,2,4]triazolo[1,5-a]pyrimidine hybrids as promising anti-inflammatory agents with COX/5-LOX/ROS/IL-6 multifunctional inhibitory activity: design, synthesis, SAR, and in silico study. (PubMed, RSC Adv) - Sep 11, 2026 - "The most potent COX-2 inhibitor 6d exhibited reasonable 5-LOX inhibitory activity (IC50 = 1.031 µM) in comparison to the selective 5-LOX inhibitor zileuton (IC50 = 0.386 µM). Moreover, 6d exhibited potent inhibitory activity against the proinflammatory cytokine IL-6 (90.9% inhibition) and ROS scavenging activity (IC50 = 34.45 µM), exceeding the two references, celecoxib and diclofenac sodium...Ultimately, docking simulations and drug-likeness studies provided insights into the potential binding scenarios within the active sites of COX-2 and 5-LOX, while also predicting the oral bioavailability and toxicity of the newly synthesized compounds. Based on these findings, the designed scaffolds can be considered as promising multitargeted anti-inflammatory candidates worthy of further exploration."
Journal • IL6 • TNFA
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Amany M Ghanim; Esraa Elazony; Hanan A Abdel-Fattah; Moataz A Shaldam; Nermine A Osman
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