偶氮-8-羟基喹啉衍生物作为阿尔茨海默病的多靶点先导候选物:单胺氧化酶和胆碱酯酶抑制剂的深入计算机研究

IF 2.6 3区 综合性期刊 Q1 MULTIDISCIPLINARY SCIENCES PLoS ONE Pub Date : 2025-01-30 eCollection Date: 2025-01-01 DOI:10.1371/journal.pone.0317261
Fatima Zahra Guerguer, Bouchra Rossafi, Oussama Abchir, Yasir S Raouf, Dhabya Bakhit Albalushi, Abdelouahid Samadi, Samir Chtita
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引用次数: 0

摘要

阿尔茨海默病的认知功能障碍是多种病理过程复杂相互作用的结果,包括关键酶如乙酰胆碱酯酶(AChE)、丁基胆碱酯酶(BuChE)和单胺氧化酶B (MAO-B)的失调。本研究提出并设计了一系列来自8-羟基喹啉(Azo-8HQ)的新分子,作为治疗AD的潜在多靶点先导候选物。研究人员进行了详尽的计算机分析,包括对接研究、ADMET分析、密度泛函数理论(DFT)研究、分子动力学模拟和随后的MM-GBSA计算,以研究这些分子与感兴趣的特定靶点的药理潜力。在分析的63个Azo-8HQ衍生物中,14c和17c两个分子与AChE、BuChE和MAO-B具有很强的亲和力,并具有良好的药代动力学特征和电子特性。分子动力学模拟证实了这些分子在靶标活性位点内的稳定性,MM-GBSA计算显示结合能较低,表明相互作用强大。基于一项旨在最小化药物开发成本和时间的深入计算研究,这些发现确定了分子14c和17c是治疗AD的有希望的多靶点候选者。未来的工作将包括这些分子的合成,然后进行深入的体外和体内测试,以验证其潜在的治疗效果。
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Potential Azo-8-hydroxyquinoline derivatives as multi-target lead candidates for Alzheimer's disease: An in-depth in silico study of monoamine oxidase and cholinesterase inhibitors.

Cognitive dysfunction in Alzheimer's disease results from a complex interplay of various pathological processes, including the dysregulation of key enzymes such as acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and monoamine oxidase B (MAO-B). This study proposes and designs a series of novel molecules derived from 8-hydroxyquinoline (Azo-8HQ) as potential multi-target lead candidates for treating AD. An exhaustive in silico analysis was conducted, encompassing docking studies, ADMET analysis, density functional theory (DFT) studies, molecular dynamics simulations, and subsequent MM-GBSA calculations to examine the pharmacological potential of these molecules with the specific targets of interest. Out of the 63 Azo-8HQ derivatives analysed, two molecules, 14c and 17c, demonstrated strong affinities for AChE, BuChE, and MAO-B, along with favourable pharmacokinetic profiles and electronic properties. Molecular dynamics simulations confirmed the stability of these molecules within the active sites of the targets, and MM-GBSA calculations revealed low binding energies, indicating robust interactions. These findings identify molecules 14c and 17c as promising multi-target candidates for the treatment of AD, based on an in-depth computational study aimed at minimizing drug development costs and time. Future work will include the synthesis of these molecules followed by in-depth in vitro and in vivo testing to validate their potential therapeutic efficacy.

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来源期刊
PLoS ONE
PLoS ONE 生物-生物学
CiteScore
6.20
自引率
5.40%
发文量
14242
审稿时长
3.7 months
期刊介绍: PLOS ONE is an international, peer-reviewed, open-access, online publication. PLOS ONE welcomes reports on primary research from any scientific discipline. It provides: * Open-access—freely accessible online, authors retain copyright * Fast publication times * Peer review by expert, practicing researchers * Post-publication tools to indicate quality and impact * Community-based dialogue on articles * Worldwide media coverage
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