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Synthesis and cholinesterase inhibitory activity of new 2-benzofuran carboxamide-benzylpyridinum salts

Publication date:

October 2018


Source:Bioorganic Chemistry, Volume 80

Author(s): Fahimeh Abedinifar, S. Morteza F. Farnia, Mohammad Mahdavi, Hamid Nadri, Alireza Moradi, Jahan B. Ghasemi, Tuba Tüylü Küçükkılınç, Loghman Firoozpour, Alireza Foroumadi

A series of benzofuran-2-carboxamide-N-benzyl pyridinium halide derivatives (6a-o) are synthesized as new cholinesterase inhibitors. The synthetic pathway involves the reaction of salicylaldehyde derivatives and ethyl bromoacetate, followed by hydrolysis and amidation with 3- and 4-picolyl amine. Subsequently, N-((pyridin-4-yl) methyl) benzofuran-2-carboxamide and substituted N-((pyridin-3-yl) methyl) benzofuran-2-carboxamides reacts with benzyl halides to afford target compounds (6a-o). The chemical structures of all derivatives were confirmed by spectroscopic methods. The studies reveal that some of the synthesized compounds are potent butyrylcholinesterase inhibitors with IC50 values in the range of 0.054–2.7 µM. In addition, good inhibitory effects on Aβ self-aggregation are observed for 6h and 6k (33.1 and 46.4% at 100 µM, respectively).
Graphical abstract




Autoren:   Author(s): Fahimeh Abedinifar, S. Morteza F. Farnia, Mohammad Mahdavi, Hamid Nadri, Alireza Moradi, Jahan B. Ghasemi, Tuba Tüylü Küçükkılınç, Loghman Firoozpour, Alireza Foroumadi
Journal:   Bioorganic Chemistry
Band:   80
Jahrgang:   2018
Seiten:   180
DOI:   10.1016/j.bioorg.2018.06.006
Erscheinungsdatum:   25.06.2018
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