CAS: 544467-07-4; Hiv-1 Integrase Inhibitor

该化合物是一种化学化合物,其独特结构包括一个附于一个苯环和二氧丁酸混合物的亚甲甲基组,该化合物具有酸性和潜在反应性功能组,使其对包括药用化学和材料科学在内的各种化学应用感兴趣.Azide组的存在表明,有可能点击化学反应,用于生物合成或聚合合成聚合物.二氧丁酸成分表明,该化合物可能表现出基多醇陶美主义,影响其再活性和稳定性.此外,该化合物的分子结构可能具有特定的溶性和极性特征,影响其在不同溶剂中的行为.

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物理性质

MSDS等安全信息

    上下游产品

    1-(3-(Azidomethyl) Phenyl) Ethanone 544467-05-2

    合成工艺路线路线简述

      📜1-(3-(溴甲基)苯基)乙酮置于sodium Hydroxide,Sodium Azide,Sodium Hydride体系中,用 1,4-二氧六环,水,丙酮,甲苯 作为反应溶剂,化学反应 1.0H,反应生成 4-[3-(叠氮基甲基)苯基]-2-羟基-4-氧代-2-丁烯酸
      参考文献:Azido-Containing Aryl β-Diketo Acid Hiv-1 Integrase Inhibitors
      标题:Azido-Containing Aryl β-Diketo Acid Hiv-1 Integrase Inhibitors
      摘要:Aryl Beta-Diketo Acids (Adk) Comprise A General Class Of Potent Hiv-1 Integrase (In) Inhibitors,Which Can Exhibit Selective Inhibition Of Strand Transfer Reactions In Extracellular Recombinant In Assays And Provide Potent Antiviral Effects In Hiv-Infected Cells. Recent Studies Have Shown That Polycyclic Aryl Or Aryl Rings Bearing Aryl-Containing Substituents Are Components Of Potent Members Of This Class. Reported Herein Is The First Use Of Azido Functionality As An Aryl Replacement In Beta-Diketo Acid In Inhibitors. The Ability Of Azido-Containing Inhibitors To Exhibit Potent Inhibition Of In And Antiviral Protection In Hiv-Infected Cells,Renders The Azide Group Of Potential Value In The Further Development Of Adk-Based In Inhibitors. (C) 2003 Elsevier Science Ltd. All Rights Reserved.
      DOI:10.1016/s0960-894X(03)00059-3

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      主要参考文献


      1: Sanchez AB, Varano GP, de Rozieres CM, Maung R, Catalan IC, Dowling CC, Sejbuk NE, Hoefer MM, Kaul M. Antiretrovirals, Methamphetamine, and HIV-1 Envelope Protein gp120 Compromise Neuronal Energy Homeostasis in Association with Various Degrees of Synaptic and Neuritic Damage. Antimicrob Agents Chemother. 2015 Oct 19;60(1):168-79. doi: 10.1128/AAC.01632-15.
      2: Mbemba G, Henry E, Delelis O, Bouger MC, Buckle M, Mouscadet JF, Hazan U, Leh H, Bury-Moné S. Biochemical properties of the xenotropic murine leukemia virus- related virus integrase. Biochimie. 2014 Dec;107 Pt B:300-9. doi: 10.1016/j.biochi.2014.09.019. Epub 2014 Sep 26. 5(4):e01318-14. doi: 10.1128/mBio.01318-14.
      4: McElrath MJ, Ballweber L, Terker A, Kreger A, Sakchalathorn P, Robinson B, Fialkow M, Lentz G, Hladik F. Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cells. Antimicrob Agents Chemother. 2010 Feb;54(2):763-72. doi: 10.1128/AAC.00891-09. Epub 2009 Nov 30. PMCID: PMC2812173

      合成参考文献


      参考文献:10.1371/journal.ppat.1003125
      摘要:Tavis JE, Cheng X, Hu Y, Totten M, Cao F, Michailidis E, Aurora R, Meyers MJ, Jacobsen EJ, Parniak MA, Sarafianos SG. The Hepatitis B Virus Ribonuclease H Is Sensitive to Inhibitors of the Human Immunodeficiency Virus Ribonuclease H and Integrase Enzymes. PLoS Pathog. 2013 Jan 22;9(1):e1003125. doi: 10.1371/journal.ppat.1003125.
      参考文献:10.1016/s0960-894x(03)00059-3
      摘要:Zhang X, Pais GC, Svarovskaia ES, Marchand C, Johnson AA, Karki RG, Nicklaus MC, Pathak VK, Pommier Y, Burke TR. Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1215–9. doi: 10.1016/s0960-894x(03)00059-3.
      参考文献:10.1124/mol.64.3.600
      摘要:Marchand C, Johnson AA, Karki RG, Pais GC, Zhang X, Cowansage K, Patel TA, Nicklaus MC, Burke TR, Pommier Y. Metal-dependent inhibition of HIV-1 integrase by beta-diketo acids and resistance of the soluble double-mutant (F185K/C280S). Mol Pharmacol. 2003 Sep;64(3):600–9. doi: 10.1124/mol.64.3.600.
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