Antioxidant evaluation of novel 3-Aryl-5-phenyloxy-1,2,4-oxadiazoles as radical scavengers: Synthesis, characterization, and ADME studies

Le résumé fourni par la source

Cell function depends on redox homeostasis, and several diseases are linked to its disruption. The relative amounts of reduced and oxidised glutathione play a major role in controlling redox balance. Redox equilibrium is essential for a number of physiological functions, including protein folding and cell signalling. Thus, redox imbalance has been linked to a number of clinical illnesses, including diabetes, cancer, and neurodegenerative diseases. Here, we designed and synthesized a new library of 3, 5-diaryl-1,2,4-oxadiazole derivatives, evaluated by scavenging the dangerous free radicals. The produced oxadiazoles are all examined by spectroscopic and micro-analytical techniques. Three assays were used to assess the antioxidant properties: total antioxidant (FRAP), DPPH (2,2-diphenyl-1-picrylhydrazyl) radicals, and nitric oxide. When nitric oxide, DPPH, and FRAP were combined, the results were nearly same. Key findings revealed that compounds 12 , 10 , and 13 exhibited superior NO scavenging activity with IC 50 values of 35.59 ± 1.3, 37.41 ± 1.1, and 40.54 ± 1.3 μM, respectively. DPPH assay results indicated potent radical scavenging activity, with IC 50 values of 67.08 ± 1.1 to 99.94 ± 1.1 μM. In the FRAP assay, compounds 15 , 18 , 11 , 10 , and 12 demonstrated the highest antioxidant activities, which were consistent with the results of the other assays. Computational predictions of the physicochemical attributes, pharmacokinetic profiles, and drug-likeness data of all the synthesized compounds indicated that our hits may be introduced as drug-like candidates because they showed appropriate criteria in medicinal chemistry and drug-likeness values which hopefully can alleviate poor biopharmaceutical properties of many antioxidants.

Ce résumé expose les affirmations des auteurs. BNTIC ne l’interprète pas comme une validation indépendante des résultats.