Synthesis and Biological Evaluation of a Series of Dithiocarbamates as New Cholinesterase Inhibitors

Abstract

In the present paper, a novel series of dithiocarbamates was synthesized via the treatment of 4-(trifluoromethyl)benzyl chloride with appropriate sodium salts of N,N-disubstituted dithiocarbamic acids. H-1 NMR, mass spectral data, and elemental analyses. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) using a modification of Ellman's spectrophotometric method. 2g (IC50=0.53 +/- 0.001 mu M) followed by compounds 2f (IC50=0.74 +/- 0.001 mu M) and 2j (IC50=0.89 +/- 0.002 mu M) when compared with donepezil (IC50=0.048 +/- 0.001 mu M). Compounds 2f and 2g were more effective than donepezil (IC50=7.88 +/- 0.52 mu M) on BuChE inhibition. Compounds 2f and 2g exhibited the inhibitory effect on BuChE with IC50 values of 1.39 +/- 0.041 and 3.64 +/- 0.072 mu M, respectively.