Related references
Note: Only part of the references are listed.
Article
Biochemistry & Molecular Biology
Donia E. Hafez et al.
Summary: Introduced a multi-targeted ligand for neurodegenerative diseases, such as Alzheimer's disease, which offers an improved therapeutic alternative compared to the traditional one-target, one-molecule approach. Certain compounds showed potential for multi-targeting by evaluating their interactions with AChE, BuChE, and MAO-B, suggesting their potential as lead structures for developing new multi-targeting anti-AD agents.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Pengxia Qin et al.
Summary: The multitarget-directed ligands approach is a potential strategy for treating Alzheimer's disease, due to its multifactorial pathology. In this study, a series of N-benzyl piperidine derivatives were designed, synthesized, and characterized for dual inhibitions of histone deacetylase (HDAC) and acetylcholinesterase (AChE). Compound d5 and d10 exhibited dual enzyme inhibitions, scavenging free radicals, chelating metal, and inhibiting A beta aggregations. Additionally, they showed promising neuroprotective activities and good AChE selectivity in PC-12 cells. These findings encourage further optimization and exploration for developing more potent analogues as potential treatments for Alzheimer's disease.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Srabanti Jana et al.
Summary: This study aimed to develop novel small molecules as selective monoamine oxidase B (MAO-B) inhibitors with cholinesterase inhibition. Compound 6m showed the best neuroprotection, with reversible selective MAO-B inhibition activity (IC50 = 11.54 +/- 0.64 nM). Compounds 6b, 6h, 6j, 6n and 6p also appeared as potent and selective MAO-B inhibitors with anti-AChE activity.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Neda Anastassova et al.
Summary: Oxidative stress plays a crucial role in the development of Parkinson's disease. Inhibition of MAO-B can enhance dopamine availability and prevent the formation of reactive oxygen species (ROS). The introduction of hydroxy and methoxy groups in a new series of benzimidazole-2-thione compounds increases their neuroprotective activity. Safety evaluation on SH-SY5Y cells and rat brain synaptosomes demonstrates their strong safety profile. Compounds 3h and 3i exhibit the most potent neuroprotective and antioxidant activity, surpassing melatonin and rasagiline. Several compounds also show significant MAO-B inhibitory effects, with 3h being the most potent. These compounds, particularly 3h, possess strong antioxidant effects against lipid peroxidation and scavenging capability against superoxide radicals. This study highlights a multifunctional compound with excellent safety profile, neuroprotective, antioxidant, and MAO-B inhibitory properties.
Article
Biochemistry & Molecular Biology
Simone Carradori et al.
Summary: Neurodegenerative diseases are multifactorial and progressive syndromes that compromise cognitive and behavioral functions. This study investigated the dual inhibitory ability of a series of resveratrol analogs against two important targets involved in neurodegeneration, and identified a compound with promising therapeutic potential.
Article
Geriatrics & Gerontology
Shishuai Wang et al.
Summary: Heat-clearing and detoxifying Chinese medicines, such as Fibraurea recisa Pierre (FRP), have been found to have potential anti-Alzheimer's disease (AD) effects. This study identified 12 components in FRP with anti-AD activities and explored the potential mechanism of action using network pharmacology and molecular docking. The results revealed that palmatine, berberine, and other alkaloids in FRP were key active ingredients for the treatment of AD. Additionally, pathways including neuroactive ligand-receptor interaction and the PI3K-Akt signaling pathway were found to be significant in FRP's anti-AD role.
FRONTIERS IN AGING NEUROSCIENCE
(2022)
Article
Biotechnology & Applied Microbiology
Na Zhang et al.
Summary: This study investigated the protective effect of Baichanting (BCT) against Parkinson's disease (PD) using an integrated strategy of network pharmacology and brain metabolomics. The results showed that BCT delayed the occurrence and development of PD by improving the brain metabolic disorder, revealing the mechanism of BCT through multitarget and multipathway treatment.
BIOMED RESEARCH INTERNATIONAL
(2022)
Article
Geriatrics & Gerontology
Chan Liu et al.
Summary: The study synthesized a novel multi-target-directed ligand (AP5) and used computational simulations and in vivo pharmacokinetic evaluations to confirm its potential. The results showed that AP5 can simultaneously bind to the peripheral and catalytic sites of AChE and has desirable pharmacokinetic characteristics and drug-likeness. AP5 can inhibit AChE activity and AChE-induced Aβ aggregation, reduce Aβ plaque deposition, suppress inflammation, and prevent neuronal and synaptic damage in Alzheimer's disease models.
FRONTIERS IN AGING NEUROSCIENCE
(2022)
Review
Chemistry, Medicinal
Ewelina Krolicka et al.
Summary: With the increasing life expectancy, there is a significant rise in the number of people suffering from neurodegenerative diseases (ND). Parkinson's disease (PD), the second most common ND after Alzheimer's disease, is characterized by motor and non-motor symptoms that severely impact patients' lives. Current therapies can only alleviate symptoms and slow down disease progression, but cannot effectively cure it. Therefore, it is important to understand the mechanism and causes of PD and find potent treatment strategies. This review focuses on chalcones and related structures as potential therapeutics for PD, exploring their enzyme inhibitory properties, anti-neuroinflammatory activity, and receptor antagonism.
Review
Pharmacology & Pharmacy
Alexander B. Pupyshev et al.
Summary: Trehalose is a promising approach for the treatment of neurodegenerative diseases through its induction of autophagy. It has anti-inflammatory, antioxidant, and neuroprotective effects, reducing the accumulation of abnormal proteins. Trehalose activates lysosome and autophagosome biogenesis pathways. However, further research is needed to understand its pharmacodynamics. Trehalose has demonstrated potential in treating diseases such as Alzheimer's, Parkinson's, and Huntington's in animal models.
PHARMACOLOGICAL RESEARCH
(2022)
Article
Medicine, General & Internal
Xinyan Wu et al.
Summary: This study identified that curcumin can treat Alzheimer's disease by regulating multiple targets and pathways through network pharmacology.
