Synthesis of new piperazine compounds and investigation of their anticholinesterase effects

Abstract

Purpose: The aim of present study is to evaluate anticholinesterase activities of some new piperazine compounds. Materials and Methods: Ten new piperazine derivatives were synthesized. Structure elucidation of the synthesized compounds was performed by spectroscopic medhods. Inhibitory activities of these compounds on acetylcholine esterase (AChE) and butrylcholine esterase (BChE) enzymes have been determined by Ellman's colorimetric assay. Enzyme kinetic studies were performed for the most active compound 2b by using Lineweaver-Burk plots. Results: The compound 2b including chloro substituent was found as the most active derivative with 82.95 %, 66.93 % and 42.63 % inhibition rates at 1 mM, 0.1 mM and 0.01 mM concentrations, respectively. Noncompetitive type of inhibition was determined for compound 2b as a result of enzyme kinetic studies. Conclusion: None of the compounds showed activity as much as standard drug donepezil. However, compound 2b and 2c displayed a promising and selective inhibitory activity against AChE.