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


ABSTRACT: The design, synthesis and assessment of ?-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 A? 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-A? 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.

SUBMITTER: Horton W 

PROVIDER: S-EPMC5282889 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature

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

Horton William W   Sood Abha A   Peerannawar Swarada S   Kugyela Nandor N   Kulkarni Aditya A   Tulsan Rekha R   Tran Chris D CD   Soule Jessica J   LeVine Harry H   Török Béla B   Török Marianna M  

Bioorganic & medicinal chemistry letters 20161124 2


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  ...[more]

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