Title : Synthesis and anticholinesterase activity of coumarin-3-carboxamides bearing tryptamine moiety - Ghanei-Nasab_2016_Eur.J.Med.Chem_121_40 |
Author(s) : Ghanei-Nasab S , Khoobi M , Hadizadeh F , Marjani A , Moradi A , Nadri H , Emami S , Foroumadi A , Shafiee A |
Ref : Eur Journal of Medicinal Chemistry , 121 :40 , 2016 |
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 muM. 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). |
PubMedSearch : Ghanei-Nasab_2016_Eur.J.Med.Chem_121_40 |
PubMedID: 27214510 |
Ghanei-Nasab S, Khoobi M, Hadizadeh F, Marjani A, Moradi A, Nadri H, Emami S, Foroumadi A, Shafiee A (2016)
Synthesis and anticholinesterase activity of coumarin-3-carboxamides bearing tryptamine moiety
Eur Journal of Medicinal Chemistry
121 :40
Ghanei-Nasab S, Khoobi M, Hadizadeh F, Marjani A, Moradi A, Nadri H, Emami S, Foroumadi A, Shafiee A (2016)
Eur Journal of Medicinal Chemistry
121 :40