BIOLOGICAL EVALUTION OF THIAZOLE DERIVATIVES BEARING DITHIOCARBAMATE MOIETY AS POTENTIAL CHOLINESTERASE INHIBITORS
Objective: This study aimed to synthesize some thiazole derivatives bearing dithiocarbamic acid esters and to evaluate their anticholinesterase activity.
Methods: 2-Chloro-N-[4-(2-methyl-4-thiazolyl)phenyl]acetamide was stirred with appropriate sodium salts of dithiocarbamic acids in acetone. The resulted compounds were elucidated using IR, 1H-NMR, and FAB+-MS spectral data. Each derivative was evaluated for its ability to inhibit acetyl cholinesterase (AChE) in vitro by using a modification of Ellmanâ€™s spectophotometric method.
Results: Two of the synthesized compounds (6b,6c) can be identified as promising anticholinesterase agent due to their inhibitory effect on ACEH with IC50 value of86.34Â±1.31, 91.74Â±1.43 respectively when compared with standard substance Donepezil (IC50 =0.054Â±0.002Î¼M) under the same experimental conditions.
Conclusion: dimethylaminoethyl/propyl substitution on Piperazine residue have a crucial influence on anticholinesterase activity.
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