| Literature DB >> 27289559 |
Zahra Najafi1, Mina Saeedi2, Mohammad Mahdavi3, Reyhaneh Sabourian4, Mahnaz Khanavi5, Maliheh Barazandeh Tehrani1, Farshad Homayouni Moghadam6, Najmeh Edraki7, Elahe Karimpor-Razkenari4, Mohammad Sharifzadeh8, Alireza Foroumadi9, Abbas Shafiee9, Tahmineh Akbarzadeh10.
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-2H-chromen-2-one (8e) exhibited the most potent anti-acetylcholinesterase (AChE) inhibitory activity (IC50=16.17μM) comparing with rivastigmine (IC50=11.07μM) as the reference drug. Also, compound 8e was assessed for its β-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.Entities:
Keywords: Acridine-chromenone; Alzheimer’s disease; Anti-cholinesterase; Docking study; Neuroprotective activity; Quinoline-chromenone; β-Secretase inhibitor
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Year: 2016 PMID： 27289559 DOI： 10.1016/j.bioorg.2016.06.001
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275