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炔丙胺:药物发现中的重要部分。

Propargylamine: an important moiety in drug discovery.

机构信息

CIQUP-IMS/Department of Chemistry & Biochemistry, Faculty of Sciences, University of Porto, Rua do Campo Alegre 687, Porto, 4169-007, Portugal.

Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, Santiago de Compostela, 15782, Spain.

出版信息

Future Med Chem. 2023 Jan;15(2):211-224. doi: 10.4155/fmc-2022-0243. Epub 2023 Feb 21.

DOI:10.4155/fmc-2022-0243
PMID:36802855
Abstract

Propargylamine is a chemical moiety whose properties have made it a widely distributed group within the fields of medicinal chemistry and chemical biology. Its particular reactivity has traditionally popularized the preparation of propargylamine derivatives using a large variety of synthetic strategies, which have facilitated the access to these compounds for the study of their biomedical potential. This review comprehensively covers and analyzes the applications that propargylamine-based derivatives have achieved in the drug discovery field, both from a medicinal chemistry perspective and from a chemical biology-oriented approach. The principal therapeutic fields where propargylamine-based compounds have made an impact are identified, and a discussion of their influence and growing potential is included.

摘要

炔丙胺是一种化学基团,其性质使其在药物化学和化学生物学领域中广泛分布。其独特的反应性使得使用各种合成策略来制备炔丙胺衍生物变得非常流行,这为研究其生物医学潜力提供了这些化合物的途径。本文全面综述和分析了基于炔丙胺的衍生物在药物发现领域中的应用,从药物化学和化学生物学的角度进行了分析。确定了基于炔丙胺的化合物产生影响的主要治疗领域,并讨论了它们的影响和不断增长的潜力。

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1
Propargylamine: an important moiety in drug discovery.炔丙胺:药物发现中的重要部分。
Future Med Chem. 2023 Jan;15(2):211-224. doi: 10.4155/fmc-2022-0243. Epub 2023 Feb 21.
2
Propargylamine as functional moiety in the design of multifunctional drugs for neurodegenerative disorders: MAO inhibition and beyond.炔丙胺作为神经退行性疾病多功能药物设计中的功能部分:单胺氧化酶抑制作用及其他。
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Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.新型炔丙胺修饰的4-氨基烷基咪唑取代嘧啶基硫脲衍生物作为治疗阿尔茨海默病多功能药物的发现。
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Propargylamine containing compounds as modulators of proteolytic cleavage of amyloid-beta protein precursor: involvement of MAPK and PKC activation.含炔丙胺的化合物作为淀粉样β蛋白前体蛋白水解切割的调节剂:涉及 MAPK 和 PKC 的激活。
J Alzheimers Dis. 2010;21(2):361-71. doi: 10.3233/JAD-2010-100150.
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Interaction of monoamine oxidase inhibitory drugs with some phospholipids.单胺氧化酶抑制药物与某些磷脂的相互作用。
J Pharm Biomed Anal. 1993 Jul;11(7):563-8. doi: 10.1016/0731-7085(93)80006-m.
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Regulation of Bcl-2 family proteins, neurotrophic factors, and APP processing in the neurorescue activity of propargylamine.炔丙胺神经保护活性中Bcl-2家族蛋白、神经营养因子及淀粉样前体蛋白加工的调控
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A gold-catalysed imine-propargylamine cascade sequence: synthesis of 3-substituted-2,5-dimethylpyrazines and the reaction mechanism.金催化的亚胺-炔丙胺串联反应:3-取代-2,5-二甲基吡嗪的合成及反应机理
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Propargylamine-derived multitarget-directed ligands: fighting Alzheimer's disease with monoamine oxidase inhibitors.丙炔胺衍生的多靶点导向配体:用单胺氧化酶抑制剂治疗阿尔茨海默病。
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Novel intramolecular rearrangement of tertiary propargylamine N-oxides.叔炔丙胺 N-氧化物的新型分子内重排
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Propargylamine-selective dual fluorescence turn-on method for post-synthetic labeling of DNA.炔丙胺选择性双荧光开启法用于 DNA 的后期合成标记。
Chem Commun (Camb). 2020 Mar 12;56(21):3199-3202. doi: 10.1039/d0cc00255k.

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Beilstein J Org Chem. 2024 Nov 6;20:2827-2833. doi: 10.3762/bjoc.20.238. eCollection 2024.
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