BIOLOGICAL EVALUTION OF THIAZOLE DERIVATIVES BEARING DITHIOCARBAMATE MOIETY AS POTENTIAL CHOLINESTERASE INHIBITORS

  • Usama Abu Mohsen Al-azhar university-Gaza

Abstract

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 Ellman'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 of86.34±1.31, 91.74±1.43 respectively when compared with standard substance Donepezil (IC50 =0.054±0.002μM) under the same experimental conditions.

Conclusion: dimethylaminoethyl/propyl substitution on Piperazine residue have a crucial influence on anticholinesterase activity.

 

Keywords: Thiazole, Dithiocarbamate, Cholinesterase inhibitors

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Author Biography

Usama Abu Mohsen, Al-azhar university-Gaza
Pharmaceutical chemistry

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How to Cite
Abu Mohsen, U. “BIOLOGICAL EVALUTION OF THIAZOLE DERIVATIVES BEARING DITHIOCARBAMATE MOIETY AS POTENTIAL CHOLINESTERASE INHIBITORS”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 7, no. 2, Dec. 2014, pp. 258-61, https://innovareacademics.in/journals/index.php/ijpps/article/view/3940.
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