双（7）-他克林衍生物作为多靶点导向配体：聚焦于抗胆碱酯酶和抗淀粉样蛋白活性。 - Suppr

Bis(7)-tacrine derivatives as multitarget-directed ligands: Focus on anticholinesterase and antiamyloid activities.

作者信息

Bolognesi Maria Laura, Bartolini Manuela, Mancini Francesca, Chiriano Gianpaolo, Ceccarini Luisa, Rosini Michela, Milelli Andrea, Tumiatti Vincenzo, Andrisano Vincenza, Melchiorre Carlo

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Bologna, Italy.

出版信息

ChemMedChem. 2010 Aug 2;5(8):1215-20. doi: 10.1002/cmdc.201000086.

DOI:10.1002/cmdc.201000086

PMID:20486153

Abstract

摘要

相似文献

Bis(7)-tacrine derivatives as multitarget-directed ligands: Focus on anticholinesterase and antiamyloid activities.双（7）-他克林衍生物作为多靶点导向配体：聚焦于抗胆碱酯酶和抗淀粉样蛋白活性。

ChemMedChem. 2010 Aug 2;5(8):1215-20. doi: 10.1002/cmdc.201000086.

New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties.新型他克林-4-氧代-4H-色烯杂合体作为治疗阿尔茨海默病的多效药物，具有胆碱能、抗氧化和β-淀粉样蛋白降低特性。

J Med Chem. 2012 Feb 9;55(3):1303-17. doi: 10.1021/jm201460y. Epub 2012 Jan 27.

Tacrine-based dual binding site acetylcholinesterase inhibitors as potential disease-modifying anti-Alzheimer drug candidates.基于他克林的双结合位点乙酰胆碱酯酶抑制剂作为有潜力的治疗阿尔茨海默病的药物候选物。

Chem Biol Interact. 2010 Sep 6;187(1-3):411-5. doi: 10.1016/j.cbi.2010.02.013. Epub 2010 Feb 16.

Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of AD.多功能他克林衍生物针对阿尔茨海默病多种疾病途径的合成与药理评价

Bioorg Med Chem Lett. 2015 Feb 15;25(4):807-10. doi: 10.1016/j.bmcl.2014.12.084. Epub 2015 Jan 6.

Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors.乙酰胆碱酯酶和丁酰胆碱酯酶识别位点的特异性靶向。新型、选择性和高效胆碱酯酶抑制剂的合理设计。

J Med Chem. 2003 Jan 2;46(1):1-4. doi: 10.1021/jm0255668.

Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.基于他克林的人类胆碱酯酶抑制剂：肽链连接衍生物的合成及其对效力和选择性的影响。

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5213-6. doi: 10.1016/j.bmcl.2008.08.076. Epub 2008 Aug 26.

From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold.从乙酰胆碱酯酶抑制剂到β-分泌酶1抑制剂：茚满酮骨架上胺基的作用。

Bioorg Med Chem Lett. 2015 Jul 15;25(14):2804-8. doi: 10.1016/j.bmcl.2015.05.002. Epub 2015 May 9.

Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as dual inhibitors for cholinesterases and amyloid beta aggregation.新型他克林-多烷氧基苯杂合体的设计、合成与评价，作为乙酰胆碱酯酶和β-淀粉样蛋白聚集的双重抑制剂。

Bioorg Med Chem. 2011 Jan 15;19(2):763-70. doi: 10.1016/j.bmc.2010.12.022. Epub 2010 Dec 13.

Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase.新型异二价他克林衍生物作为胆碱酯酶抑制剂，对丁酰胆碱酯酶具有显著的选择性。

J Med Chem. 2006 Dec 14;49(25):7540-4. doi: 10.1021/jm060742o.

Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.吡喃并[3,2-c]喹啉-6-氯他克林杂合物作为一类新型的乙酰胆碱酯酶和β-淀粉样蛋白导向的抗阿尔茨海默病化合物。

J Med Chem. 2009 Sep 10;52(17):5365-79. doi: 10.1021/jm900859q.

引用本文的文献

Bis(7)-harmine derivatives as potential multi-target anti-Alzheimer agents.双（7）-哈尔明衍生物作为潜在的多靶点抗阿尔茨海默病药物。

Front Chem. 2025 Jan 29;13:1545908. doi: 10.3389/fchem.2025.1545908. eCollection 2025.

Discovery of Dual Aβ/Tau Inhibitors and Evaluation of Their Therapeutic Effect on a Model of Alzheimer's Disease.发现双重 Aβ/Tau 抑制剂及其在阿尔茨海默病模型中的治疗效果评估。

ACS Chem Neurosci. 2022 Dec 7;13(23):3314-3329. doi: 10.1021/acschemneuro.2c00357. Epub 2022 Nov 29.

The Antiviral Drug Tilorone Is a Potent and Selective Inhibitor of Acetylcholinesterase.抗病毒药物噻洛酮是一种强效且选择性的乙酰胆碱酯酶抑制剂。

Chem Res Toxicol. 2021 May 17;34(5):1296-1307. doi: 10.1021/acs.chemrestox.0c00466. Epub 2021 Jan 5.

Molecular Targets of Bis (7)-Cognitin and Its Relevance in Neurological Disorders: A Systematic Review.双（7）-认知素的分子靶点及其在神经系统疾病中的相关性：一项系统综述。

Front Neurosci. 2019 May 9;13:445. doi: 10.3389/fnins.2019.00445. eCollection 2019.

Multi-Target-Directed Ligands and other Therapeutic Strategies in the Search of a Real Solution for Alzheimer's Disease.多靶点导向配体及其他治疗策略在阿尔茨海默病治疗中的探索。

Curr Neuropharmacol. 2014 Jan;12(1):2-36. doi: 10.2174/1570159X113116660047.

Multi-target design strategies in the context of Alzheimer's disease: acetylcholinesterase inhibition and NMDA receptor antagonism as the driving forces.阿尔茨海默病背景下的多靶点设计策略：以乙酰胆碱酯酶抑制和N-甲基-D-天冬氨酸受体拮抗作用为驱动力

Neurochem Res. 2014 Oct;39(10):1914-23. doi: 10.1007/s11064-014-1250-1. Epub 2014 Feb 4.

Sphingosylphosphorylcholine attenuated β-amyloid production by reducing BACE1 expression and catalysis in PC12 cells.鞘氨醇磷酸胆碱通过降低 PC12 细胞中 BACE1 的表达和催化活性来减少β-淀粉样肽的产生。

Neurochem Res. 2011 Nov;36(11):2083-90. doi: 10.1007/s11064-011-0532-0. Epub 2011 Jun 15.

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Bis(7)-tacrine derivatives as multitarget-directed ligands: Focus on anticholinesterase and antiamyloid activities.

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