鉴定降低细胞内 tau 水平的二氢吡啶类化合物。
Identification of dihydropyridines that reduce cellular tau levels.
机构信息
Department of Pathology and the Life Sciences Institute, University of Michigan, 210 Washtenaw Ave., Ann Arbor, MI 48109, USA.
出版信息
Chem Commun (Camb). 2011 Jan 7;47(1):529-31. doi: 10.1039/c0cc02253e. Epub 2010 Nov 16.
Abstract
A series of dihydropyridines were identified that have an effect on the accumulation of tau, an important target in Alzheimer's disease. The dihydropyridine collection was expanded using the Hantzsch multicomponent reaction to develop preliminary structure-activity relationships.
摘要
一系列二氢吡啶类化合物被鉴定出来，它们对tau 的积累有影响，tau 是阿尔茨海默病的一个重要靶点。使用 Hantzsch 多组分反应扩展了二氢吡啶库，以开发初步的结构-活性关系。
相似文献
1
Identification of dihydropyridines that reduce cellular tau levels.鉴定降低细胞内 tau 水平的二氢吡啶类化合物。
Chem Commun (Camb). 2011 Jan 7;47(1):529-31. doi: 10.1039/c0cc02253e. Epub 2010 Nov 16.
2
Optimization of diastereomeric dihydropyridines as antimalarials.作为抗疟药物的非对映二氢吡啶的优化。
Eur J Med Chem. 2024 Sep 5;275:116599. doi: 10.1016/j.ejmech.2024.116599. Epub 2024 Jun 18.
3
Four-component synthesis of 1,2-dihydropyridine derivatives and their evaluation as anticancer agents.1,2-二氢吡啶衍生物的四组分合成及其作为抗癌剂的评价。
Med Chem. 2012 May;8(3):392-400. doi: 10.2174/1573406411208030392.
4
CoMFA and CoMSIA studies of 1,2-dihydropyridine derivatives as anticancer agents.1,2-二氢吡啶衍生物作为抗癌剂的 CoMFA 和 CoMSIA 研究。
Med Chem. 2012 May;8(3):372-83. doi: 10.2174/157340612800786598.
5
One-pot synthesis of 4,6-diaryl-2-oxo(imino)-1,2-dihydropyridine-3-carbonitrile; a New Scaffold for p38alpha MAP kinase inhibition.一锅法合成4,6-二芳基-2-氧代（亚氨基）-1,2-二氢吡啶-3-腈；一种用于抑制p38α丝裂原活化蛋白激酶的新型骨架。
J Comb Chem. 2010 Jul 12;12(4):559-65. doi: 10.1021/cc1000488.
6
Microwave-assisted combinatorial synthesis of hexa-substituted 1,4-dihydropyridines scaffolds using one-pot two-step multicomponent reaction followed by a S-alkylation.采用一锅两步多组分反应随后进行S-烷基化的方法，微波辅助合成六取代1,4-二氢吡啶支架。
J Comb Chem. 2008 May-Jun;10(3):436-41. doi: 10.1021/cc700194b. Epub 2008 Apr 16.
7
Synthesis, antibacterial and antimycobacterial activities of some new 4-aryl/heteroaryl-2,6-dimethyl-3,5-bis-N-(aryl)-carbamoyl-1,4-dihydropyridines.一些新型 4-芳基/杂芳基-2,6-二甲基-3,5-双-N-(芳基)甲脒-1,4-二氢吡啶的合成、抗菌和抗分枝杆菌活性。
Eur J Med Chem. 2011 May;46(5):1564-71. doi: 10.1016/j.ejmech.2011.02.003. Epub 2011 Mar 5.
8
Synthesis of new tripodal Hantzsch 1,4-dihydropyridines under solvent-free condition and their conversion to the corresponding tripodal pyridines.无溶剂条件下新型三足 Hantzsch 1,4-二氢吡啶的合成及其转化为相应的三足吡啶。
Mol Divers. 2010 Nov;14(4):809-13. doi: 10.1007/s11030-009-9171-7. Epub 2009 Jul 4.
9
Multicomponent reactions in crop protection chemistry.作物保护化学中的多组分反应。
Bioorg Med Chem. 2020 May 15;28(10):115471. doi: 10.1016/j.bmc.2020.115471. Epub 2020 Mar 31.
10
Design, Synthesis, and Biological Evaluation of 1,4-dihydropyridine Derivatives as Potent Antitubercular Agents.作为强效抗结核药物的1,4 - 二氢吡啶衍生物的设计、合成及生物学评价
Chem Biol Drug Des. 2015 Sep;86(3):370-7. doi: 10.1111/cbdd.12502. Epub 2015 Jan 9.
引用本文的文献
1
Water compatible silica supported iron trifluoroacetate and trichloroacetate: as prominent and recyclable Lewis acid catalysts for solvent-free green synthesis of hexahydroquinoline-3-carboxamides.水相兼容的二氧化硅负载三氟乙酸铁和三氯乙酸铁：作为用于无溶剂绿色合成六氢喹啉-3-甲酰胺的卓越且可循环的路易斯酸催化剂。
RSC Adv. 2023 Aug 4;13(34):23431-23448. doi: 10.1039/d3ra03542e.
2
1,4-Dihydropyridine: synthetic advances, medicinal and insecticidal properties.1,4 - 二氢吡啶：合成进展、药用及杀虫特性
RSC Adv. 2022 Oct 12;12(45):29253-29290. doi: 10.1039/d2ra04589c. eCollection 2022 Oct 11.
3
Inhibitors of heat shock protein 70 (Hsp70) with enhanced metabolic stability reduce tau levels.热休克蛋白 70（Hsp70）抑制剂增强代谢稳定性可降低 tau 水平。
Bioorg Med Chem Lett. 2021 Jun 1;41:128025. doi: 10.1016/j.bmcl.2021.128025. Epub 2021 Apr 9.
4
Intercepted-Knoevenagel condensation for the synthesis of unsymmetrical fused-tricyclic 4-pyrans.用于合成不对称稠合三环4-吡喃的截获-Knoevenagel缩合反应
Tetrahedron. 2019 Oct 25;75(43). doi: 10.1016/j.tet.2019.130606. Epub 2019 Sep 17.
5
Tau Protein Squired by Molecular Chaperones During Alzheimer's Disease.阿尔茨海默病中分子伴侣对 Tau 蛋白的稳定作用。
J Mol Neurosci. 2018 Nov;66(3):356-368. doi: 10.1007/s12031-018-1174-3. Epub 2018 Sep 28.
6
Transcriptional Inhibitors Identified in a 160,000-Compound Small-Molecule DUX4 Viability Screen.在一项针对160,000种化合物的小分子DUX4活力筛选中鉴定出的转录抑制剂。
J Biomol Screen. 2016 Aug;21(7):680-8. doi: 10.1177/1087057116651868. Epub 2016 May 31.
7
Lanthanide and asymmetric catalyzed syntheses of sterically hindered 4-isoxazolyl-1,4-dihydropyridines and 4-isoxazolyl-quinolones.镧系元素与空间位阻4-异恶唑基-1,4-二氢吡啶和4-异恶唑基喹诺酮的不对称催化合成
Tetrahedron Lett. 2016 Jan 20;57(3):423-425. doi: 10.1016/j.tetlet.2015.12.038.
8
The molecular diversity scope of 1,3-indandione in organic synthesis.1,3-茚二酮在有机合成中的分子多样性范围
Mol Divers. 2016 Feb;20(1):111-52. doi: 10.1007/s11030-015-9589-z. Epub 2015 May 10.
9
Specific calpain inhibition by calpastatin prevents tauopathy and neurodegeneration and restores normal lifespan in tau P301L mice.钙蛋白酶抑制蛋白特异性抑制钙蛋白酶可预防 tau 病和神经退行性变，并恢复 tau P301L 小鼠的正常寿命。
J Neurosci. 2014 Jul 9;34(28):9222-34. doi: 10.1523/JNEUROSCI.1132-14.2014.
10
Pharmacological tuning of heat shock protein 70 modulates polyglutamine toxicity and aggregation.药物调节热休克蛋白 70 可调节多聚谷氨酰胺毒性和聚集。
ACS Chem Biol. 2012 Sep 21;7(9):1556-64. doi: 10.1021/cb300166p. Epub 2012 Jun 22.
本文引用的文献
1
Chemical manipulation of hsp70 ATPase activity regulates tau stability.热休克蛋白70（hsp70）ATP酶活性的化学调控可调节tau蛋白稳定性。
J Neurosci. 2009 Sep 30;29(39):12079-88. doi: 10.1523/JNEUROSCI.3345-09.2009.
2
Enantioselective organocatalytic Hantzsch synthesis of polyhydroquinolines.多氢喹啉的对映选择性有机催化汉茨希合成
Org Lett. 2009 Jul 16;11(14):2957-9. doi: 10.1021/ol901114f.
3
Chaperone signalling complexes in Alzheimer's disease.阿尔茨海默病中的伴侣蛋白信号复合物
J Cell Mol Med. 2009 Apr;13(4):619-30. doi: 10.1111/j.1582-4934.2008.00557.x.
4
Synthesis of new acridines and hydrazones derived from cyclic beta-diketone for cytotoxic and antiviral evaluation.新型吖啶及环β - 二酮衍生腙的合成用于细胞毒性和抗病毒评估。
Eur J Med Chem. 2009 Sep;44(9):3680-6. doi: 10.1016/j.ejmech.2009.04.001. Epub 2009 Apr 8.
5
Tau pathophysiology in neurodegeneration: a tangled issue.神经退行性变中的 Tau 病理生理学：一个复杂的问题。
Trends Neurosci. 2009 Mar;32(3):150-9. doi: 10.1016/j.tins.2008.11.007. Epub 2009 Jan 21.
6
Blocking Abeta42 accumulation delays the onset and progression of tau pathology via the C terminus of heat shock protein70-interacting protein: a mechanistic link between Abeta and tau pathology.通过热休克蛋白70相互作用蛋白的C末端阻断淀粉样蛋白β42的积累可延迟tau蛋白病变的发生和进展：淀粉样蛋白β与tau蛋白病变之间的机制联系。
J Neurosci. 2008 Nov 19;28(47):12163-75. doi: 10.1523/JNEUROSCI.2464-08.2008.
7
Tau mutations in neurodegenerative diseases.神经退行性疾病中的tau基因突变。
J Biol Chem. 2009 Mar 6;284(10):6021-5. doi: 10.1074/jbc.R800013200. Epub 2008 Oct 22.
8
The natively unfolded character of tau and its aggregation to Alzheimer-like paired helical filaments.tau蛋白的天然未折叠特性及其聚集成阿尔茨海默病样双螺旋丝。
Biochemistry. 2008 Oct 7;47(40):10526-39. doi: 10.1021/bi800783d. Epub 2008 Sep 11.
9
Untangling tau hyperphosphorylation in drug design for neurodegenerative diseases.在神经退行性疾病药物设计中解析tau蛋白过度磷酸化问题
Nat Rev Drug Discov. 2007 Jun;6(6):464-79. doi: 10.1038/nrd2111.
10
The high-affinity HSP90-CHIP complex recognizes and selectively degrades phosphorylated tau client proteins.高亲和力的HSP90-CHIP复合物识别并选择性降解磷酸化的tau客户蛋白。
J Clin Invest. 2007 Mar;117(3):648-58. doi: 10.1172/JCI29715. Epub 2007 Feb 15.
Zotero 插件