| Title : Novel tacrine-coumarin hybrids linked to 1,2,3-triazole as anti-Alzheimer's compounds: In vitro and in vivo biological evaluation and docking study - Najafi_2018_Bioorg.Chem_83_303 |
| Author(s) : Najafi Z , Mahdavi M , Saeedi M , Karimpour-Razkenari E , Edraki N , Sharifzadeh M , Khanavi M , Akbarzadeh T |
| Ref : Bioorg Chem , 83 :303 , 2018 |
|
Abstract :
A new series of tacrine-coumarin hybrids linked to 1,2,3-triazole were designed, synthesized, and tested as potent dual binding site cholinesterase inhibitors (ChEIs) for the treatment of Alzheimer's disease (AD). Among them, compound 8e was the most potent anti-AChE derivative (IC50=27nM) and compound 8m displayed the best anti-BChE activity (IC50=6nM) much more active than tacrine and donepezil as the reference drugs. Compound 8e was also evaluated for its BACE1 inhibitory activity and neuroprotectivity against PC12 cells exposed to Abeta25-35 which indicated low activity. Finally, in vivo studies by Morris water maze task showed that compound 8e significantly reversed scopolamine-induced memory deficit in rats. |
| PubMedSearch : Najafi_2018_Bioorg.Chem_83_303 |
| PubMedID: 30396115 |
Najafi Z, Mahdavi M, Saeedi M, Karimpour-Razkenari E, Edraki N, Sharifzadeh M, Khanavi M, Akbarzadeh T (2018)
Novel tacrine-coumarin hybrids linked to 1,2,3-triazole as anti-Alzheimer's compounds: In vitro and in vivo biological evaluation and docking study
Bioorg Chem
83 :303
Najafi Z, Mahdavi M, Saeedi M, Karimpour-Razkenari E, Edraki N, Sharifzadeh M, Khanavi M, Akbarzadeh T (2018)
Bioorg Chem
83 :303