Synthesis, Anticholinesterase, and Antibacterial Activity of N-Aroyl-a-Aminoacrylic Acid Dialkylaminoalkylamides

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作者
V. O. Topuzyan
Z. G. Alebyan
R. V. Paronikyan
机构
[1] A. L. Mndzhoyan Institute of Fine Organic Chemistry,Science Technology Center of Organic and Pharmaceutical Chemistry, National Academy of Sciences of the Republic of Armenia
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关键词
α-aminoacrylic acid derivatives; anticholinesterase properties; iodomethylates of dialkylaminoalkyl amides; AChE; BChE;
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摘要
N-Aroyl-α-aminoacrylic acid 2-(dialkylamino)alkylamides and their quaternary ammonium salts were synthesized and their physicochemical properties were determined. Results obtained from studies of their interactions with human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) are presented. IC50 values (concentrations producing 50% inhibition of the rate of cholinesterase hydrolysis of 0.1 mM acetylthiocholine) were determined for all the compounds synthesized. The results show that all the compounds synthesized had anticholinesterase properties, mainly specific in relation to BChE. Data on the antibacterial properties of the synthesized compounds are also presented.
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页码:304 / 308
页数:4
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