importazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: importazole
• 英文别名: IPZ；N-(1-phenylethyl)-2-pyrrolidin-1-ylquinazolin-4-amine
• 化学式: C₂₀H₂₂N₄
• 分子量: 318.421
• InChiKey: HKGJEZIGDHFJFL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  41
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  α-苯乙胺 在 sodium hydride 、 sodium carbonate 作用下， 以 N,N-二甲基甲酰胺 、 正丁醇 为溶剂， 反应 3.5h， 生成 importazole
  参考文献：
  名称：

  支架变形导致2，4-二氨基喹啉和氨基吡唑并嘧啶作为ATP合成途径的抑制剂而演化† ‡

  摘要：

  贝达喹啉作为抗结核药治疗多药耐药性结核病的成功证实了ATP合成途径，特别是ATP合酶是有吸引力的靶标。但是，由于其在临床中的使用以及与利福平之间的药物相互作用而受到的局限性促使人们进行了研究努力，以鉴定具有不同作用机制的其他ATP合成抑制剂。生化分析用于筛选阿斯利康的公司化合物集合，以鉴定分枝杆菌ATP合成的抑制剂。高通量筛选导致鉴定出2,4-二氨基喹唑啉为ATP合成途径的抑制剂。建立了喹唑啉的构效关系，并利用该知识将喹唑啉核心转变为喹啉和吡唑并嘧啶，以扩大化学多样性的范围。变形的支架在抑制哺乳动物线粒体ATP合成方面显示出十倍的酶效价提高和超过一百倍的选择性提高。这些新型化合物具有杀菌作用，并显示出结核分枝杆菌急性小鼠模型中的结核分枝杆菌。

  DOI：

  10.1039/c5md00589b

文献信息

• USE OF COMPOUNDS FOR PREPARING ANTI-TUBERCULOSIS AGENTS
  申请人：Wynne Graham Michael

  公开号：US20100317607A1

  公开（公告）日：2010-12-16

  Compounds of a compound of compound of general formula (I) wherein X 1 , X 2 , A, R 1 R 2 , R 3 and R 4 are as defined herein; are useful as anti-mycobacterial agents, especially agents for the treatment of tuberculosis.

  在本文中，化合物的一般公式（I）中，X1、X2、A、R1、R2、R3和R4的定义如上所述；这些化合物可用作抗分枝杆菌剂，特别是用于治疗结核病的药剂。
• Compositions and Methods for Reducing Cancer Cell Proliferation and Modulating Importin-Beta Function
  申请人：The Regents of the University of California

  公开号：US20130225611A1

  公开（公告）日：2013-08-29

  The present disclosure provides methods of reducing proliferation of cancer cells. The methods include contacting the cancer cells with a 2,4-diaminoquinazoline compound. Also provided are methods of modulating importin-beta function (e.g., importin-beta-mediated nuclear import) in eukaryotic cells. The methods include contacting the eukaryotic cells with a 2,4-diaminoquinazoline compound. Pharmaceutical formulations that include a 2,4-diaminoquinazoline compound are also provided.
• COMPOSITIONS AND METHODS FOR INHIBITION OF NUCLEAR-PENETRATING ANTIBODIES
  申请人：Yale University

  公开号：US20210137960A1

  公开（公告）日：2021-05-13

  Compositions and methods of treating autoimmune diseases by administering a subject in need thereof an effective amount of an inhibitor of the importin pathway are also provided. Typically, the autoimmune disease has one or more symptoms or pathologies dependent on or otherwise caused by nuclear penetrating antibodies, for example, nuclear penetrating autoantibodies. In specific embodiments, the autoimmune disease is scleroderma or a form of lupus, for example systemic lupus erythematosus. In preferred embodiments, the inhibitor of the importin pathway is a macrocyclic lactone such as an avermectin or a milbemycin. Compositions, formulations, and dosage forms including an effective amount of the macrocyclic lactones to reduce nuclear localization of a nuclear penetrating antibody are also provided. The compositions can be employed in the disclosed methods. Exemplary dosages ranges and dosage regimens are also provided.
• ANTIBACTERIAL COMPOUNDS AND USES THEREOF
  申请人：The Children's Medical Center Corporation

  公开号：US20220023270A1

  公开（公告）日：2022-01-27

  Provided herein are compositions and methods for the treatment of infections resulting from antibiotic-resistant strains of bacteria.
• [EN] USE OF COMPOUNDS FOR PREPARING ANTI-TUBERCULOSIS AGENTS<br/>[FR] UTILISATION DE COMPOSÉS POUR LA PRÉPARATION D'AGENTS ANTI-TUBERCULOSE
  申请人：SUMMIT CORP PLC

  公开号：WO2009001060A2

  公开（公告）日：2008-12-31

  [EN] Compounds of a compound of compound of general formula (I) wherein X1, X2, A, R1 R2, R3 and R4 are as defined herein; are useful as anti-mycobacterial agents, especially agents for the treatment of tuberculosis.
  [FR] L'invention concerne des composés représentés par la formule générale (I) dans laquelle X1, X2, A, R1 R2, R3 et R4 sont tels que définis présentement. Ces composés sont utiles comme agents antimycobactériens, notamment comme agents pour le traitement de la tuberculose.