1498922-66-9Relevant articles and documents
Synthesis and biological evaluation of a series of dithiocarbamates as new cholinesterase inhibitors
Altintop, Mehlika D.,Gurkan-Alp, A. Selen,Oezkay, Yusuf,Kaplancbox, Zafer A.
, p. 571 - 576 (2013/09/02)
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 1H 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. The most potent AChE inhibitor was found as compound 2g (IC50 = 0.53 ± 0.001 μM) followed by compounds 2f (IC50 = 0.74 ± 0.001 μM) and 2j (IC50 = 0.89 ± 0.002 μM) when compared with donepezil (IC50 = 0.048 ± 0.001 μM). Compounds 2f and 2g were more effective than donepezil (IC50 = 7.88 ± 0.52 μM) 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 μM, respectively.
