Altintop_2013_Arch.Pharm.(Weinheim)_346_571

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. The chemical structures of the compounds were elucidated by (1) H NMR, mass spectral data, and elemental analyses. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BCHE) using a modification of Ellman's spectrophotometric method. The most potent AChE inhibitor was found as compound 2g (IC50 = 0.53 +/- 0.001 microM) followed by compounds 2f (IC50 = 0.74 +/- 0.001 microM) and 2j (IC50 = 0.89 +/- 0.002 microM) when compared with donepezil (IC50 = 0.048 +/- 0.001 microM). Compounds 2f and 2g were more effective than donepezil (IC50 = 7.88 +/- 0.52 microM) on BCHE inhibition. Compounds 2f and 2g exhibited the inhibitory effect on BCHE with IC50 values of 1.39 +/- 0.041 and 3.64 +/- 0.072 microM, respectively.