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In silico assessment of the metabolism and its safety significance of multitarget propargylamine ASS234.多靶点炔丙胺ASS234代谢及其安全性意义的计算机模拟评估
CNS Neurosci Ther. 2018 Oct;24(10):981-983. doi: 10.1111/cns.12990. Epub 2018 May 28.
2
Upregulation of Antioxidant Enzymes by ASS234, a Multitarget Directed Propargylamine for Alzheimer's Disease Therapy.ASS234对阿尔茨海默病治疗的多靶点导向炔丙胺对抗氧化酶的上调作用
CNS Neurosci Ther. 2016 Sep;22(9):799-802. doi: 10.1111/cns.12590. Epub 2016 Jul 6.
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Neuroinflammation Signaling Modulated by ASS234, a Multitarget Small Molecule for Alzheimer's Disease Therapy.神经炎症信号被 ASS234 调节，ASS234 是一种用于治疗阿尔茨海默病的多靶小分子药物。
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In-vitro and in-vivo evaluation of the modulatory effects of the multitarget compound ASS234 on the monoaminergic system.多靶点化合物ASS234对单胺能系统调节作用的体外和体内评价
J Pharm Pharmacol. 2017 Mar;69(3):314-324. doi: 10.1111/jphp.12697. Epub 2017 Jan 30.
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Wnt signaling pathway, a potential target for Alzheimer's disease treatment, is activated by a novel multitarget compound ASS234.Wnt信号通路是阿尔茨海默病治疗的一个潜在靶点，被一种新型多靶点化合物ASS234激活。
CNS Neurosci Ther. 2014 Jun;20(6):568-70. doi: 10.1111/cns.12269. Epub 2014 Apr 8.
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Modulation of Heat Shock Response Proteins by ASS234, Targeted for Neurodegenerative Diseases Therapy.通过靶向神经退行性疾病治疗的 ASS234 对热休克反应蛋白的调节。
Chem Res Toxicol. 2018 Sep 17;31(9):839-842. doi: 10.1021/acs.chemrestox.8b00192. Epub 2018 Aug 27.
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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。
Future Med Chem. 2015;7(5):609-29. doi: 10.4155/fmc.15.12.
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Zn(II)-Catalyzed synthesis of piperidines from propargyl amines and cyclopropanes.锌（II）催化由炔丙胺和环丙烷合成哌啶
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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
Chem Commun (Camb). 2014 May 7;50(35):4567-70. doi: 10.1039/c4cc01485e.
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Design, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.新型多奈哌齐-吲哚基杂合物作为多效胆碱酯酶/单胺氧化酶抑制剂用于潜在治疗阿尔茨海默病的设计、合成、药理学评价、定量构效关系分析、分子模拟及药物代谢动力学/药物毒性预测
Eur J Med Chem. 2014 Mar 21;75:82-95. doi: 10.1016/j.ejmech.2013.12.028. Epub 2014 Jan 27.

引用本文的文献

1
Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy.ASS234亮点：一种用于阿尔茨海默病治疗的新型且有前景的治疗药物。
Neural Regen Res. 2020 Jan;15(1):30-35. doi: 10.4103/1673-5374.262679.

本文引用的文献

1
Alzheimer's Disease, the "One-Molecule, One-Target" Paradigm, and the Multitarget Directed Ligand Approach.阿尔茨海默病、"一个分子，一个靶点"范式与多靶点导向配体方法。
ACS Chem Neurosci. 2018 Mar 21;9(3):401-403. doi: 10.1021/acschemneuro.8b00069. Epub 2018 Feb 21.
2
In-vitro and in-vivo evaluation of the modulatory effects of the multitarget compound ASS234 on the monoaminergic system.多靶点化合物ASS234对单胺能系统调节作用的体外和体内评价
J Pharm Pharmacol. 2017 Mar;69(3):314-324. doi: 10.1111/jphp.12697. Epub 2017 Jan 30.
3
The proof-of-concept of ASS234: Peripherally administered ASS234 enters the central nervous system and reduces pathology in a male mouse model of Alzheimer disease.ASS234的概念验证：经外周给药的ASS234进入中枢神经系统，并减轻阿尔茨海默病雄性小鼠模型中的病理变化。
J Psychiatry Neurosci. 2017 Jan;42(1):59-69. doi: 10.1503/jpn.150209.
4
Upregulation of Antioxidant Enzymes by ASS234, a Multitarget Directed Propargylamine for Alzheimer's Disease Therapy.ASS234对阿尔茨海默病治疗的多靶点导向炔丙胺对抗氧化酶的上调作用
CNS Neurosci Ther. 2016 Sep;22(9):799-802. doi: 10.1111/cns.12590. Epub 2016 Jul 6.
5
Establishing best practise in the application of expert review of mutagenicity under ICH M7.在国际人用药品注册技术协调会（ICH）M7指导原则下建立致突变性专家评审应用的最佳实践。
Regul Toxicol Pharmacol. 2015 Oct;73(1):367-77. doi: 10.1016/j.yrtph.2015.07.018. Epub 2015 Aug 4.
6
Wnt signaling pathway, a potential target for Alzheimer's disease treatment, is activated by a novel multitarget compound ASS234.Wnt信号通路是阿尔茨海默病治疗的一个潜在靶点，被一种新型多靶点化合物ASS234激活。
CNS Neurosci Ther. 2014 Jun;20(6):568-70. doi: 10.1111/cns.12269. Epub 2014 Apr 8.
7
Multipotent, permeable drug ASS234 inhibits Aβ aggregation, possesses antioxidant properties and protects from Aβ-induced apoptosis in vitro.多功能、可渗透的药物 ASS234 抑制 Aβ 聚集，具有抗氧化特性，并能防止体外 Aβ 诱导的细胞凋亡。
Curr Alzheimer Res. 2013 Oct;10(8):797-808. doi: 10.2174/15672050113109990151.
8
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease.多奈哌齐和 N-[(5-(苄氧基)-1-甲基-1H-吲哚-2-基)甲基]-N-甲基丙-2-炔-1-胺杂合体的合成、生物评价和分子模拟作为治疗阿尔茨海默病的新型多效胆碱酯酶/单胺氧化酶抑制剂。
J Med Chem. 2011 Dec 22;54(24):8251-70. doi: 10.1021/jm200853t. Epub 2011 Nov 15.

In silico assessment of the metabolism and its safety significance of multitarget propargylamine ASS234.

作者信息

Ramos Eva, Marco-Contelles José, López-Muñoz Francisco, Romero Alejandro

机构信息

Faculty of Veterinary Medicine, Department of Pharmacology and Toxicology, Complutense University of Madrid, Madrid, Spain.

Laboratory of Medicinal Chemistry, Institute of General Organic Chemistry (CSIC) Madrid, Madrid, Spain.

出版信息

CNS Neurosci Ther. 2018 Oct;24(10):981-983. doi: 10.1111/cns.12990. Epub 2018 May 28.

DOI:10.1111/cns.12990
PMID:29808538
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6490147/
Abstract
摘要