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An overview on the synthesis of carbohydrate-based molecules with biological activity related to neurodegenerative diseases.

ABSTRACT: In the context of the search for multitarget drugs with improved efficacy against neurodegenerative disorders, carbohydrate derivatives have emerged as promising candidates for Alzheimer's therapy. Herein we describe the synthesis and biological evaluation of several classes of sugar-based compounds, where most of them contain heterocyclic aromatic moieties that bear known biological properties and high affinity for the cholinesterase active site. This general idea led to the synthesis of compounds with high inhibitory potency against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), enzymatic selectivity and combined properties such as antioxidant and neuroprotection, in addition to the absence of toxicity.

SUBMITTER: Lopes JPB

PROVIDER: S-EPMC8672812 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature

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An overview on the synthesis of carbohydrate-based molecules with biological activity related to neurodegenerative diseases.

Lopes João Paulo B JPB Silva Luana L Lüdtke Diogo S DS

RSC medicinal chemistry 20210908 12

In the context of the search for multitarget drugs with improved efficacy against neurodegenerative disorders, carbohydrate derivatives have emerged as promising candidates for Alzheimer's therapy. Herein we describe the synthesis and biological evaluation of several classes of sugar-based compounds, where most of them contain heterocyclic aromatic moieties that bear known biological properties and high affinity for the cholinesterase active site. This general idea led to the synthesis of compou ...[more]

PMID: 35028560

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Project description:The identification of protective agents for the treatment of neurodegenerative diseases is the mainstay therapeutic goal to modify the disease course and arrest the irreversible disability progression. Pharmacological therapies synergistically targeting multiple pathogenic pathways, including oxidative stress, mitochondrial dysfunction, and inflammation, are prime candidates for neuroprotection. Combination or synergistic therapy with melatonin, whose decline correlates with altered sleep/wake cycle and impaired glymphatic "waste clearance" system in neurodegenerative diseases, has a great therapeutic potential to treat inflammatory neurodegenerative states. Despite the protective outcomes observed in preclinical studies, mild or poor outcomes were observed in clinical settings, suggesting that melatonin combinations promoting synergistic actions at appropriate doses might be more suitable to treat multifactorial neurodegenerative disorders. In this review, we first summarize the key melatonin actions and pathways contributing to cell protection and its therapeutic implication in Alzheimer's disease (AD), Parkinson's disease (PD), and multiple sclerosis (MS). We remark the major controversies in the field, mostly generated by the lack of a common consensus for the optimal dosing, molecular targets, and toxicity. Then, we review the literature investigating the efficacy of melatonin combinations with approved or investigational neuroprotective agents and of melatonin-containing hybrid molecules, both in vitro and in animal models of AD, PD, and MS, as well as the efficacy of add-on melatonin in clinical settings. We highlight the rationale for such melatonin combinations with a focus on the comparison with single-agent treatment and on the assays in which an additive or a synergistic effect has been achieved. We conclude that a better characterization of the mechanisms underlying such melatonin synergistic actions under neuroinflammation at appropriate doses needs to be tackled to advance successful clinical translation of neuroprotective melatonin combination therapies or melatonin-based hybrid molecules.

Dataset Information

An overview on the synthesis of carbohydrate-based molecules with biological activity related to neurodegenerative diseases.

Publications

An overview on the synthesis of carbohydrate-based molecules with biological activity related to neurodegenerative diseases.

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