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Synthesis and anticholinesterase activity of coumarin-3-carboxamides bearing tryptamine moiety.

Abstract：

: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 IC50 value 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).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Ghanei-Nasab S,Khoobi M,Hadizadeh F,Marjani A,Moradi A,Nadri H,Emami S,Foroumadi A,Shafiee A

doi

10.1016/j.ejmech.2016.05.014

subject

Has Abstract

pub_date

2016-10-04 00:00:00

pages

40-46

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30391-9

journal_volume

121

pub_type

杂志文章

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