A new class of substituted 8-hydroxyquinoline derivatives containing oxadiazole ring 4a-e were synthesised through multi step reactions. The structures of the newly synthesised compounds were confirmed by LC-MS, 1 H NMR, Elemental Analysis and FTIR-spectral analysis. The second step involved the synthesis of esters (2a-e) by using the base NaOH, which reduced the reaction time drastically as well as improved the yield when compared to the reported methods. The newly synthesised compounds were evaluated for antioxidant, and angiotensin-I-converting enzyme (ACE-I) inhibitory activities. The compound 4d emerged as the most effective antioxidant agent against R-tocopherol, Mannitol, BHT and BHA. Among the compounds tested, 4c, 4d and 4e exhibited ACE-I inhibitory activity with IC50 253.089, 1022.660 and 1101.950 ± 2µM respectively. Docking simulation further supported the probable binding conformation with ACE-I active site for 4c.
Loading....