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23
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6
Objectives: In this study, we aimed to synthesize fourteen different 2-[(1-methyl-1H-tetrazole-5-yl) thio]-1-(substituted phenyl)ethanone derivatives (1–14) and to investigate their anticholinesterase activities. Method: 1-(Substituted phenyl)-2-[(1-methyl-1H-tetrazol-5-yl) thio]ethanone compounds were synthesized by reacting 1-methyl-1H-tetrazol-5-thiol with some phenacyl bromide derivatives. The structures of the obtained compounds were elucidated using IR, 1H-NMR, 13C-NMR and FAB+-MS spectral data and elemental analyses results. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman’s spectrophotometric method. Results: The compound 2 and 3 were found as the most active compounds due to their inhibitory effect on AChE with inhibition percentages of 29.56 and 24.38%. Conclusion: The compounds with electron donating substituents methyl and chloro at the third position of phenyl residue have exhibited the highest anticholinesterase activity. Key words: Tetrazole, cholinesterase inhibitors
Objectives: In this study, we aimed to synthesize fourteen different 2-[(1-methyl-1H-tetrazole-5-yl) thio]-1-(substituted phenyl)ethanone derivatives (1-14) and to investigate their anticholinesterase activities. Method: 1-(Substituted phenyl)-2-[(1-methyl-1H-tetrazole-5-yl) thio]ethanone compounds were synthesized by reacting 1-methyl-1H-tetrazole-5-thiol with some phenacyl bromide derivatives. The structures of the obtained compounds were elucidated using IR, 1H-NMR, 13C-NMR and FAB+-MS spectral data and elemental analyses results. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman's spectrophotometric method. Results: The compounds 2 and 3 were found as the most active compounds due to their inhibitory effect on AChE with inhibition percentages of 29.56 and 24.38%. Conclusion: The compounds with electron donating substituents methyl and chlorine at the third position of phenyl residue have exhibited the highest anticholinesterase activity. Key words: tetrazole, cholinesterase inhibitors
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