Biological Evalution of Thiazole Derivatives Bearing Dithiocarbamate Moiety as Potential Cholinesterase Inhibitors
Year: 2014
Type: article
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, 1 H-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 IC 50 value of86.34±1.31, 91.74±1.43 respectively when compared with standard substance Donepezil (IC 50 =0.054±0.002μM) under the same experimental conditions. Conclusion : dimethylaminoethyl/propyl substitution on Piperazine residue have a crucial influence on anticholinesterase activity.
Author: Usama Abu Mohsen
Institution: Al-Azhar University – Gaza
Language: English
Subfield: Pharmacology (medical)
Field: Medicine
Domain: Health Sciences
Open Access status: diamond
OpenAlex ID: W1551091270