375830-77-6Relevant academic research and scientific papers
Synthesis and anticholinesterase activity and cytotoxicity of novel amide derivatives
Altintop, Mehlika Dilek,Kaplancikli, Zafer Asim,Ozdemir, Ahmet,Turan-Zitouni, Guelhan,Temel, Halide Edip,Akalin, Guelsen
, p. 112 - 116 (2012/04/10)
In the present study, some amide derivatives were synthesized and their potential anticholinesterase properties were investigated. N-(Benzothiazol-2-yl) -2-[(5-amino/methyl-1,3,4-thiadiazol-2-yl)thio]acetamide derivatives were obtained by nucleophilic substitution of 2-chloro-N-(benzothiazole-2-yl) acetamide derivatives with appropriate 1,3,4-thiadiazole-2-thioles. The chemical structures of the compounds were elucidated by 1H-NMR, 13C-NMR and FAB+-MS spectral data and elemental analyses. Each amide derivative was evaluated for its ability to inhibit AChE and BuChE using a modification of Ellman's spectrophotometric method. The compounds were also investigated for their cytotoxic properties using MTT assay. 2-(5-Amino-1,3,4-thiadiazol-2-yl)thio-N-(benzothiazol-2-yl)acetamide derivatives have anticholinesterase activity, whereas 2-(5-methyl-1,3,4-thiadiazol-2-yl) thio-N-(benzothiazol-2-yl)acetamide derivatives have no inhibitory effect on enzyme activity. Among these compounds, it is clear that compound IIh is the most potent derivative. Among these new compounds, compound IIh is the most potent inhibitor of AChE and BuChE with an IC50 value of 66±0.71μg/mL and 48.75±2.48μg/mL, respectively.
