European Journal of Medicinal Chemistry p. 40 - 46 (2016)
Update date:2022-07-29
Topics:
Ghanei-Nasab, Samaneh
Khoobi, Mehdi
Hadizadeh, Farzin
Marjani, Azam
Moradi, Alireza
Nadri, Hamid
Emami, Saeed
Foroumadi, Alireza
Shafiee, Abbas
A number of N-(2-(1H-indol-3-yl)ethyl)-2-oxo-2H-chromene-3-carboxamides were synthesized and tested against AChE and BuChE. The in?vitro assessment of the synthesized compounds 4a-o revealed that most of them had significant activity toward AChE. The SAR study demonstrated that the introduction of benzyloxy moiety on the 7-position of coumarin scaffold can improve the anti-AChE activity. The best result was obtained with 7-(4-fluorobenzyl)oxy moiety in the case of compound 4o, displaying IC50value of 0.16?μM. Based on the docking study of AChE, the prototype compound 4o was laid across the active site and occupied both peripheral anionic site (PAS) and catalytic anionic site (CAS).
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