多奈哌齐+色酮+褪黑素杂合体作为治疗阿尔茨海默病的有希望的药物。
Donepezil + chromone + melatonin hybrids as promising agents for Alzheimer's disease therapy.
机构信息
a Neurosciences intégratives et cliniques, Pôle Chimie Organique et Thérapeutique , University Bourgogne Franche-Comté , Besançon , France.
b Faculty of Science, Department of Chemistry , University of Hradec Kralove , Hradec Kralove , Czech Republic.
出版信息
J Enzyme Inhib Med Chem. 2019 Dec;34(1):479-489. doi: 10.1080/14756366.2018.1545766.
We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC = 11.90 ± 0.05 nM), moderate hAChE (IC = 1.73 ± 0.34 μM), hMAO A (IC = 2.78 ± 0.12 μM), and MAO B (IC = 21.29 ± 3.85 μM) inhibition, while keeping a strong antioxidant power (3.04 TE, ORAC test). Consequently, the results reported here support the development of new multitarget Donepezil + Chromone + Melatonin hybrids, such as compound 14n, as a potential drug for AD patients cure.
我们在此描述了新的多奈哌齐+色酮+褪黑素杂合体的设计、多组分合成和生物学研究，作为治疗阿尔茨海默病（AD）的潜在药物。我们已经确定化合物 14n 是一种很有前途的多靶点小分子，具有很强的 BuChE 抑制作用（IC=11.90±0.05 nM）、适度的 hAChE（IC=1.73±0.34 μM）、hMAO A（IC=2.78±0.12 μM）和 MAO B（IC=21.29±3.85 μM）抑制作用，同时保持很强的抗氧化能力（3.04 TE，ORAC 测试）。因此，这里报道的结果支持开发新的多靶点多奈哌齐+色酮+褪黑素杂合体，如化合物 14n，作为 AD 患者治疗的潜在药物。
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