| Title : Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids - Najafi_2016_Bioorg.Chem_67_84 |
| Author(s) : Najafi Z , Saeedi M , Mahdavi M , Sabourian R , Khanavi M , Tehrani MB , Moghadam FH , Edraki N , Karimpor-Razkenari E , Sharifzadeh M , Foroumadi A , Shafiee A , Akbarzadeh T |
| Ref : Bioorg Chem , 67 :84 , 2016 |
|
Abstract :
A novel series of acridine-chromenone and quinoline-chromenone hybrids were designed, synthesized, and evaluated as anti-Alzheimer's agents. All synthesized compounds were evaluated as cholinesterases (ChEs) inhibitors and among them, 7-(4-(6-chloro-2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylamino)phenoxy)-4-methyl-2 H-chromen-2-one (8e) exhibited the most potent anti-acetylcholinesterase (AChE) inhibitory activity (IC50=16.17muM) comparing with rivastigmine (IC50=11.07muM) as the reference drug. Also, compound 8e was assessed for its beta-secretase (BACE1) inhibitory and neuroprotective activities which demonstrated satisfactory results. It should be noted that both kinetic study on the inhibition of AChE and molecular modeling revealed that compound 8e interacted simultaneously with both the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. |
| PubMedSearch : Najafi_2016_Bioorg.Chem_67_84 |
| PubMedID: 27289559 |
Najafi Z, Saeedi M, Mahdavi M, Sabourian R, Khanavi M, Tehrani MB, Moghadam FH, Edraki N, Karimpor-Razkenari E, Sharifzadeh M, Foroumadi A, Shafiee A, Akbarzadeh T (2016)
Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids
Bioorg Chem
67 :84
Najafi Z, Saeedi M, Mahdavi M, Sabourian R, Khanavi M, Tehrani MB, Moghadam FH, Edraki N, Karimpor-Razkenari E, Sharifzadeh M, Foroumadi A, Shafiee A, Akbarzadeh T (2016)
Bioorg Chem
67 :84