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Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents



Synthesis and application of β-carbolines as novel multi-functional anti-Alzheimer's disease agents



Bioorganic and Medicinal Chemistry Letters 27(2): 232-236



The design, synthesis and assessment of β-carboline core-based compounds as potential multifunctional agents against several processes that are believed to play a significant role in Alzheimer's disease (AD) pathology, are described. The activity of the compounds was determined in Aβ self-assembly (fibril and oligomer formation) and cholinesterase (AChE, BuChE) activity inhibition, and their antioxidant properties were also assessed. To obtain insight into the mode of action of the compounds, HR-MS studies were carried out on the inhibitor-Aβ complex formation and molecular docking was performed on inhibitor-BuChE interactions. While several compounds exhibited strong activities in individual assays, compound 14 emerged as a promising multi-target lead for the further structure-activity relationship studies.

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Accession: 058953740

Download citation: RISBibTeXText

PMID: 27923619

DOI: 10.1016/j.bmcl.2016.11.067


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