Synthesis characterization and evaluation of novel triazole based analogs as a acetylcholinesterase and a-glucosidase inhibitors

A series of novel triazole analogs (10a-k) bearing piperidine were synthesized in an aprotic solvent on the most effective pharmacophore with acetylcholinesterase (AChE) and a-glucosidase inhibitory activity. Triazole analogs (10a-k) were obtained in excellent yields (75-90 %) and characterized by EI-MS, IR, 13C NMR and 1H NMR. The newly synthesized triazole analogs (10a-k) showed potent AChE inhibitory activity in the range of Ki = 0.0155 +/- 1.25 mu M to 0.557 +/- 0.50 mu M, IC50 = 0.031 +/- 0.85 to 0.537 +/- 0.76 mu M than Eserine (0.04 +/- 0.001 mu M) having strong electron-withdrawing fluorine group on the pyridine ring was recorded as a most potent inhibitor of AChE while (%) inhibition against a-glucosidase was ranging between 52.36 +/- 1.67 to 85.35 +/- 1.39. The kinetic study predicted that triazole analogs (10a-k) followed the un-competitive and mixed type of inhibition against AChE. In silico molecular docking was performed at the active site of the AChE co-crystal structure (PDB ID:1NEN). The results of molecular docking corelate will with the experimental findings. CO, 2023 The Author(s). Published by Elsevier B.V. on behalf of King Saud University.