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Article Dans Une Revue Journal of Medicinal Chemistry Année : 2021

β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy

Résumé

The natural β-carboline alkaloids display similarities with neurotransmitters that can be favorably exploited to design bioactive and bioavailable drugs for Alzheimer's Disease (AD) therapy. Several AD targets are currently and intensively being investigated, divided in different hypotheses: mainly the cholinergic, the Amyloid β (Aβ) and the Tau hypotheses. To date, only symptomatic treatments are available involving acetylcholinesterase and NMDA inhibitors. Based on plethoric single-target structure-activity relationship studies, the βcarboline scaffold was identified as a powerful tool for fostering activity and molecular interactions with a wide range of AD-related targets. This knowledge can undoubtedly be used to design multitarget-directed ligands (MTDL), a highly relevant strategy preferred in the context of multifactorial pathology with intricated etiology such as AD. In this review, we first individually discussed the AD targets of the β-carbolines and then we focused on the multitarget strategies dedicated to the deliberate design of new efficient scaffolds.
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Dates et versions

hal-04020932 , version 1 (09-03-2023)

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Aurélien Beato, Anthonin Gori, Benjamin Boucherle, Marine Peuchmaur, Romain Haudecoeur. β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy. Journal of Medicinal Chemistry, 2021, 64 (3), pp.1392-1422. ⟨10.1021/acs.jmedchem.0c01887⟩. ⟨hal-04020932⟩
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