European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 283, С. 117066 - 117066
Опубликована: Ноя. 27, 2024
Язык: Английский
European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 283, С. 117066 - 117066
Опубликована: Ноя. 27, 2024
Язык: Английский
European Journal of Medicinal Chemistry, Год журнала: 2022, Номер 238, С. 114464 - 114464
Опубликована: Май 20, 2022
Язык: Английский
Процитировано
90Molecules, Год журнала: 2024, Номер 29(9), С. 2127 - 2127
Опубликована: Май 3, 2024
Neurodegeneration is a gradual decay process leading to the depletion of neurons in both central and peripheral nervous systems, ultimately resulting cognitive dysfunctions deterioration brain functions, alongside decline motor skills behavioral capabilities. Neurodegenerative disorders (NDs) impose substantial socio-economic strain on society, aggravated by advancing age world population absence effective remedies, predicting negative future. In this context, urgency discovering viable therapies critical and, despite significant efforts medicinal chemists developing potential drug candidates exploring various small molecules as therapeutics, regrettably, truly treatment yet be found. Nitrogen heterocyclic compounds, particularly those containing indole nucleus, which has emerged privileged scaffold, have attracted particular attention for variety pharmacological applications. This review analyzes rational design strategy adopted different research groups development anti-neurodegenerative indole-based compounds modulate molecular targets involved NDs, with reference most recent advances between 2018 2023.
Язык: Английский
Процитировано
17European Journal of Medicinal Chemistry, Год журнала: 2021, Номер 215, С. 113278 - 113278
Опубликована: Фев. 16, 2021
Язык: Английский
Процитировано
78Journal of Medicinal Chemistry, Год журнала: 2022, Номер 65(13), С. 8550 - 8595
Опубликована: Июнь 27, 2022
A person suspected of having Alzheimer's disease (AD) is clinically diagnosed for the presence principal biomarkers, especially misfolded amyloid-beta (Aβ) and tau proteins in brain regions. Existing radiotracer diagnostic tools, such as PET imaging, are expensive have limited availability primary patient screening pre-clinical animal studies. To change status quo, small-molecular near-infrared (NIR) probes been rapidly developed, which may serve an inexpensive, handy imaging tool to comprehend dynamics pathogenic progression AD assess therapeutic efficacy vivo. This Perspective summarizes biochemistry Aβ then focuses on structurally diverse NIR with coverages their spectroscopic properties, binding affinity toward species, theranostic effectiveness. With summarized information perspective discussions, we hope that this paper a guiding designing novel vivo fluoroprobes capabilities future.
Язык: Английский
Процитировано
53International Journal of Biological Macromolecules, Год журнала: 2025, Номер unknown, С. 140436 - 140436
Опубликована: Янв. 1, 2025
Язык: Английский
Процитировано
1European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 249, С. 115145 - 115145
Опубликована: Янв. 23, 2023
Язык: Английский
Процитировано
22Journal of Enzyme Inhibition and Medicinal Chemistry, Год журнала: 2023, Номер 38(1)
Опубликована: Фев. 20, 2023
Alzheimer's disease (AD), a persistent neurological dysfunction, has an increasing prevalence with the aging of world and seriously threatens health elderly. Although there is currently no effective treatment for AD, researchers have not given up, are committed to exploring pathogenesis AD possible therapeutic drugs. Natural products attracted considerable attention owing their unique advantages. One molecule can interact multiple AD-related targets, thus having potential be developed in multi-target drug. In addition, they amenable structural modifications increase interaction decrease toxicity. Therefore, natural derivatives that ameliorate pathological changes should intensively extensively studied. This review mainly presents research on AD.
Язык: Английский
Процитировано
21Phytomedicine Plus, Год журнала: 2023, Номер 3(2), С. 100439 - 100439
Опубликована: Март 30, 2023
Alzheimer's disease (AD) is a neurodegenerative with cognitive and memory decline. Due to the lack of effective treatment for AD, there an interest in finding novel compounds treat AD. The leaves Adhatoda vasica Nees (AV) exhibited anti-AD effects known be rich pyrroloquinazoline alkaloids. However, role alkaloids as was not explored. Therefore, present study aimed isolate active through bioactivity guided fractionation from AV explore their effect. Column chromatography dichloromethane (DCM) fraction methanolic extract used AV. isolated were characterized by TLC, HPLC, ATR, HRMS, NMR techniques. In-silico, studies performed investigate interaction cholinesterase enzymes (AChE BuChE). Further, in-vitro assays carried out evaluate AChE, BuChE, Aβ inhibition properties. Propidium iodide displacement assay know selectivity at AChE PAS site. Furthermore, in-vivo improvement against scopolamine-induced amnesia induced neurotoxicity rats. A couple leads identified fractionation, such vasicinone (VAS) vasicine (VA) responsible DCM fraction. In-silico that both stable interactions BuChE sites. VAS VA inhibited aggregation effectively displaced propidium showed administration significantly improved dysfunction scopolamine impairments Besides, recovered hippocampal cell density AD Moreover, did show any sign toxicity. revealed acts potent agent it similar potency profile impairment Both possess strong potential preclinical development natural drugs anti-AD.
Язык: Английский
Процитировано
20Drug Development Research, Год журнала: 2023, Номер 84(8), С. 1624 - 1651
Опубликована: Сен. 11, 2023
Alzheimer's disease (AD) is a progressive age-related neurodegenerative brain disorder, which leads to loss of memory and other cognitive dysfunction. The underlying mechanisms AD pathogenesis are very complex still not fully explored. Cholinergic neuronal loss, accumulation amyloid plaque, metal ions dyshomeostasis, tau hyperphosphorylation, oxidative stress, neuroinflammation, mitochondrial dysfunction major hallmarks AD. current treatment options for acetylcholinesterase inhibitors (donepezil, rivastigmine, galantamine) NMDA receptor antagonists (memantine). These FDA-approved drugs mainly provide symptomatic relief without addressing the pathological aspects progression. So, there an urgent need novel drug development that only addresses basic but also shows neuroprotective property. Various research groups across globe working on multifunctional agents amelioration using different core scaffolds their design, carbamate among them. Rivastigmine was first investigated management. fragment, scaffold act as potential inhibitor acetylcholinesterase. In this review, we summarize last 10 years conducted modification with substituents primarily target ChE inhibition, reduce modulate Aβ aggregation.
Язык: Английский
Процитировано
17The Journal of Organic Chemistry, Год журнала: 2022, Номер 87(10), С. 6730 - 6741
Опубликована: Май 12, 2022
Multicomponent synthesis of biologically relevant S-benzyl dithiocarbamates from para-quinone methides, amines, and carbon disulfide are described under catalyst additive-free conditions. The reactions proceeded at room temperature in a short span time with excellent yields. One the synthesized compounds, 3e showed considerable acetylcholinesterase (AChE) inhibitory (51.70 + 5.63% 20 μm) antioxidant (63.52 ± 1.15 activities.
Язык: Английский
Процитировано
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