CAS: 338967-87-6; 3-(2,4-Dichloro-5-Methoxyphenyl)-2-Mercaptoquinazolin-4(3H)-One

该化合物是一个小分子,以其作为线粒体分解的选择性抑制剂的作用而著称,主要针对对线粒体裂变至关重要的宫内相关蛋白1 (Drp1),通过抑制Drp1, Mdivi-1能够影响线粒体形态和功能,使其成为与线粒体动力和相关疾病有关的研究的宝贵工具.该化合物具有潜在的...

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CAS号610-14-0 2-硝基苯甲酰氯 | CAS号98446-49-2 2,4-二氯-5-甲氧基苯胺 | CAS号1449294-63-6 N-(2,4-dichloro...

合成工艺路线路线简述

    📜2,4-二氯-5-甲氧基苯胺置于吡啶,Palladium 10% On Activated Carbon,氢气,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,20.0 °C,100.0 Kpa 条件下,反应 16.5H,反应生成3-(2,4-二氯-5-甲氧基苯基)-2,3-二氢-2-硫代-4(1H)-喹唑啉酮
    参考文献:Development Of 2-Thioxoquinazoline-4-One Derivatives As Dual And Selective Inhibitors Of Dynamin-Related Protein 1 (Drp1) And Puromycin-Sensitive Aminopeptidase (Psa)
    标题:Development Of 2-Thioxoquinazoline-4-One Derivatives As Dual And Selective Inhibitors Of Dynamin-Related Protein 1 (Drp1) And Puromycin-Sensitive Aminopeptidase (Psa)
    摘要:已知的dynamin相关蛋白1(drp1)抑制剂--3-(2,4-二氯-5-甲氧苯基)-2-噻唑啉酮(mdivi-1),近期还被报道显示出强大的嘌呤霉素敏感性氨基肽酶(psa)抑制活性.在此,我们报道了mdivi-1衍生物的结构开发,合成化合物的构效关系(sar)分析,以及结构相关的psa特异性抑制剂3-(2,6-二乙基苯基)喹唑啉-2,4-二酮(paq-22),旨在识别抑制活性的关键结构特征,从而开发针对drp1的选择性抑制剂,Drp1是治疗亨廷顿病的潜在靶点.在合成化合物中,3-(4-氯-3-甲氧苯基)-2-噻唑啉酮(10G)表现出比mdivi-1更强大的drp1抑制活性,并对drp1显示出高度选择性优于psa.
    Doi:10.1248/cpb.C14-00333

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    主要参考文献


    1: Kanda H, Liu S, Iida T, Yi H, Huang W, Levitt RC, Lubarsky DA, Candiotti KA, Hao S. Inhibition of Mitochondrial Fission Protein Reduced Mechanical Allodynia and Suppressed Spinal Mitochondrial Superoxide Induced by Perineural Human Immunodeficiency Virus gp120 in Rats. Anesth Analg. 2015 Sep 28. [Epub ahead of print] doi: 10.1016/j.ejphar.2015.04.056. Epub 2015 May 16. doi: 10.1007/s11064-015-1604-3. Epub 2015 May 13. doi: 10.1016/j.brainres.2015.03.033. Epub 2015 Mar 24. doi: 10.1681/ASN.2014080750. Epub 2015 Feb 2. doi: 10.1097/CCM.0000000000000817.
    10: Qian W, Salamoun J, Wang J, Roginskaya V, Van Houten B, Wipf P. The combination of thioxodihydroquinazolinones and platinum drugs reverses platinum resistance in tumor cells by inducing mitochondrial apoptosis independent of Bax and Bak. Bioorg Med Chem Lett. 2015 Feb 15;25(4):856-63. doi: 10.1016/j.bmcl.2014.12.072. Epub 2014 Dec 30.
    11: Yeon JY, Min SH, Park HJ, Kim JW, Lee YH, Park SY, Jeong PS, Park H, Lee DS, Kim SU, Chang KT, Koo DB. Mdivi-1, mitochondrial fission inhibitor, impairs developmental competence and mitochondrial function of embryos and cells in pigs. J Reprod Dev. 2015;61(2):81-9. doi: 10.1262/jrd.2014-070. Epub 2014 Dec 12.

    合成参考文献


    参考文献:10.4103/0366-6999.198922
    摘要:Liu JD, Chen HJ, Wang DL, Wang H, Deng Q. Pim-1 Kinase Regulating Dynamics Related Protein 1 Mediates Sevoflurane Postconditioning-induced Cardioprotection. Chin Med J (Engl). 2017 Feb 05;130(3):309–17.
    参考文献:10.1186/s12933-017-0501-2|10.1186/s12933-017-0540-8
    摘要:Ding M, Dong Q, Liu Z, Liu Z, Qu Y, Li X, Huo C, Jia X, Fu F, Wang X. Erratum to: Inhibition of dynamin-related protein 1 protects against myocardial ischemia–reperfusion injury in diabetic mice. Cardiovascular Diabetology. 2017 May 04;16(1):60. doi: 10.1186/s12933-017-0540-8.
    参考文献:10.1093/hmg/ddy156
    摘要:Denton K, Mou Y, Xu CC, Shah D, Chang J, Blackstone C, Li XJ. Impaired mitochondrial dynamics underlie axonal defects in hereditary spastic paraplegias. Hum Mol Genet. 2018 Jul 15;27(14):2517–30.
    参考文献:10.1016/j.tiv.2018.05.001
    摘要:Yin J, Guo J, Zhang Q, Cui L, Zhang L, Zhang T, Zhao J, Li J, Middleton A, Carmichael PL, Peng S. Doxorubicin-induced mitophagy and mitochondrial damage is associated with dysregulation of the PINK1/parkin pathway. Toxicol In Vitro. 2018 Sep;51():1–10. doi: 10.1016/j.tiv.2018.05.001.
    参考文献:10.1155/2019/7329131
    摘要:Wu Y, Yao Y, Ke H, Ying L, Wu Y, Zhao G, Lu Z. Mdivi-1 Protects CD4+ T Cells against Apoptosis via Balancing Mitochondrial Fusion-Fission and Preventing the Induction of Endoplasmic Reticulum Stress in Sepsis. Mediators of Inflammation. 2019 May 16;2019():1–14. doi: 10.1155/2019/7329131.
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