SYNTHESIS AND CHARACTERIZATION OF 4-METHYLCOUMARIN DERIVATIVES AS ANTI-CHOLINESTERASE INHIBITORS

Abstract

The objective of the present work was to synthesize 4-methylcoumarin derivatives and evaluate anti-cholinesterase activity (in vitro) of the compounds. 4-Methyl coumarin derivatives was synthesized using the Pechmann synthesis using resorcinol, and ethylacetoacetate. The anti-cholinesterase activity of the synthesized compounds was studied by modified Ellman’s method and the percent inhibition and IC50 was calculated. The yield of the compounds was in the range of 65-69%. All the compounds were soluble in chloroform and DMSO whereas insoluble in water. The synthesized derivatives were able to inhibit AChE activity dose dependently form 21.98 to 70.93%. The IC50 was calculated from inhibition percentage and was found to be 97.34 mM, 8.16 mM, 5.67 mM, 13.21 mM and 12.42 mM for C1 to C5 respectively. The inhibition of cholinesterase enzyme prevents the breakdown of acetylcholine into its component’s choline and acetyl CoA.