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

Autor: V. O. Topuzyan, R. V. Paronikyan, Z. G. Alebyan
Rok vydání: 2015
Předmět:
Zdroj: Pharmaceutical Chemistry Journal. 49:304-308
ISSN: 1573-9031
0091-150X
DOI: 10.1007/s11094-015-1274-0
Popis: 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.
Databáze: OpenAIRE