Synthesis, Biological Activity Studies And Molecular Modeling Studies Of Chalcone Compounds With Methyl Group

Abstract

A series of chalcone derivatives were synthesized as a result of the Claisen-Schmidt condensation of different aldehydes with CH3 groups with 4-piperazineacetophenone. Anticholinesterase (AChE and BChE) inhibitory activity and antidiabetes (α-amylase and α-glucosidaze) inhibitory activities of the synthesized compounds were examined. While compound 1 is the most active molecule in AChE (16.29±0.44 IC50 µM), BChE (10.19±0.04 IC50 µM) and α-amylase (105.51±0.24 IC50 µM) inhibitor activities; Compound 5 was found to be the most active molecule in α-glucosidase inhibitor activity. In silico and molecular docking studies of all molecules were performed. According to molecular docking results, all molecules were found to be more active than the reference compounds.