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Inhibitions of monoamine oxidases and acetylcholinesterase by 1-methyl, 5-phenyl substituted thiosemicarbazones: Synthesis, biochemical, and computational investigations

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Abstract A series of eleven 1-methyl, 5-phenyl substituted thiosemicarbazones (MT1–MT11) with the phenyl ring substitutions were prepared and investigated for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE).… Click to show full abstract

Abstract A series of eleven 1-methyl, 5-phenyl substituted thiosemicarbazones (MT1–MT11) with the phenyl ring substitutions were prepared and investigated for their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE). [4-(dimethylamino) phenyl]methylidene}-N-methylhydrazine-1-carbothioamide (MT5) inhibited MAO-B potently with an IC50 of 8.77 µM. Potencies for MAO-B increased in the order N(CH3)2 in MT5 >  OCH3 in MT3 >  Br in MT9. Most of the 11 compounds weakly inhibited AChE by

Keywords: inhibitions monoamine; monoamine oxidases; phenyl; phenyl substituted; methyl phenyl; substituted thiosemicarbazones

Journal Title: Process Biochemistry
Year Published: 2020

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