Journal
BIOORGANIC CHEMISTRY
Volume 67, Issue -, Pages 84-94Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2016.06.001
Keywords
Acridine-chromenone; Alzheimer's disease; Anti-cholinesterase; Docking study; Neuroprotective activity; Quinoline-chromenone; beta-Secretase inhibitor
Funding
- Research Council of Tehran University of Medical Sciences [94-03-33-30167]
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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)phe noxy)-4-methyl-2H-chromen-2-one (8e) exhibited the most potent anti-acetylcholinesterase (AChE) inhibitory activity (IC50 = 16.17 mu M) comparing with rivastigmine (IC50 = 11.07 mu M) 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. (C) 2016 Elsevier Inc. All rights reserved.
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