| Title : 3-Aryl Coumarin Derivatives Bearing Aminoalkoxy Moiety as Multi-Target-Directed Ligands against Alzheimer's Disease - Abdshahzadeh_2019_Chem.Biodivers_16_e1800436 |
| Author(s) : Abdshahzadeh H , Golshani M , Nadri H , Saberi Kia I , Abdolahi Z , Forootanfar H , Ameri A , Tuylu Kucukkilinc T , Ayazgok B , Jalili-Baleh L , Sadat Ebrahimi SE , Moghimi S , Haririan I , Khoobi M , Foroumadi A |
| Ref : Chem Biodivers , 16 :e1800436 , 2019 |
|
Abstract :
Two series of novel coumarin derivatives, substituted at 3 and 7 positions with aminoalkoxy groups, are synthesized, characterized, and screened. The effect of amine substituents and the length of cross-linker are investigated in acetyl- and butyrylcholinesterase (AChE and BuChE) inhibition. Target compounds show moderate to potent inhibitory activities against AChE and BuChE. 3-(3,4-Dichlorophenyl)-7-[4-(diethylamino)butoxy]-2H-chromen-2-one (4y) is identified as the most potent compound against AChE (IC50 =0.27 mum). Kinetic and molecular modeling studies affirmed that compound 4y works in a mixed-type way and interacts simultaneously with the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. In addition, compound 4y blocks beta-amyloid (Abeta) self-aggregation with a ratio of 44.11 % at 100 mum and significantly protects PC12 cells from H2 O2 -damage in a dose-dependent manner. |
| PubMedSearch : Abdshahzadeh_2019_Chem.Biodivers_16_e1800436 |
| PubMedID: 30957958 |
Abdshahzadeh H, Golshani M, Nadri H, Saberi Kia I, Abdolahi Z, Forootanfar H, Ameri A, Tuylu Kucukkilinc T, Ayazgok B, Jalili-Baleh L, Sadat Ebrahimi SE, Moghimi S, Haririan I, Khoobi M, Foroumadi A (2019)
3-Aryl Coumarin Derivatives Bearing Aminoalkoxy Moiety as Multi-Target-Directed Ligands against Alzheimer's Disease
Chem Biodivers
16 :e1800436
Abdshahzadeh H, Golshani M, Nadri H, Saberi Kia I, Abdolahi Z, Forootanfar H, Ameri A, Tuylu Kucukkilinc T, Ayazgok B, Jalili-Baleh L, Sadat Ebrahimi SE, Moghimi S, Haririan I, Khoobi M, Foroumadi A (2019)
Chem Biodivers
16 :e1800436