Cholinesterase inhibitors for the treatment of Alzheimer's disease: Synthesis, biological analysis and molecular docking study of sulphur containing heterocyclic analogues

Abstract

In synthetic medicinal chemistry thiophene and their analogues play a vital role due to the wide range of pharmacological properties. In current studies, we have synthesized a new class of thiophene-bearing sulfonamide analogues (1–11) as cholinesterase inhibitors. These newly synthesized upon esterification, hydrazide formation and finally through sulfonamide mode of synthesis and were characterized through 1H, 13C NMR and HREI-MS spectroscopic techniques. Synthesized analogues showed an excellent to moderate cholinesterase inhibitory potential. Analogues 10, 7, 9 and 11 showed an excellent potency against cholinesterase inhibition as compared to standard Donepezil. The binding interactions of the most potent analogues were confirmed through molecular docking studies. All Compounds were verified for cytotoxicity against 3T3 mouse fibroblast cell line and detected non-toxic.