2-[4-[(Z)-4-[4-(4,5-dihydro-1H-imidazol-2-yl)phenoxy]but-2-enoxy]phenyl]-4,5-dihydro-1H-imidazole

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 2-[4-[(Z)-4-[4-(4,5-dihydro-1H-imidazol-2-yl)phenoxy]but-2-enoxy]phenyl]-4,5-dihydro-1H-imidazole
• 化学式: C₂₂H₂₄N₄O₂
• 分子量: 376.458
• InChiKey: DTXPQWHAEILBLI-UPHRSURJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  28
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  67.2
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  乙二胺 、 以 甲醇 为溶剂， 生成 2-[4-[(Z)-4-[4-(4,5-dihydro-1H-imidazol-2-yl)phenoxy]but-2-enoxy]phenyl]-4,5-dihydro-1H-imidazole
  参考文献：
  名称：

  Pentamidine Congeners. 2. 2-Butene-Bridged Aromatic Diamidines and Diimidazolines as Potential Anti-Pneumocystis carinii Pneumonia Agents

  摘要：

  We have synthesized cis and trans geometric isomers 1-8 as semirigid congeners of pentamidine. Compounds 1-4 were more potent than pentamidine in treating Pneumocystis carinii pneumonia in immunosuppressed rats. These compounds also demonstrated no clinical toxicity or histopathologic abnormalities. Introduction of methoxy substituents meta to the amidine or imidazoline groups of the phenyl rings as in compounds 5-8 generally resulted in compounds with decreased anti-P. carinii activity and increased toxicity to the host. Compounds 1-4 were evaluated as DNA binders. These compounds showed greater affinity for poly(dA).poly(dT) than for calf thymus DNA. The cis isomers, 1 and 2, demonstrated greater affinity for DNA than their trans counterparts 3 and 4. This difference in DNA binding affinity, however, did not reflect in a corresponding difference in the anti-P. carinii activity of these compounds.

  DOI：

  10.1021/jm00052a014

文献信息

• Amidine derivatives for treating amyloidosis
  申请人：Chalifour J. Robert

  公开号：US20070021483A1

  公开（公告）日：2007-01-25

  The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a therapeutic amount of an amidine compound. Among the compounds for use according to the invention are those according to the following Formula, such that, when administered, amyloid fibril formation, neurodegeneration, or cellular toxicity is reduced or inhibited:

  本发明涉及在治疗与淀粉样相关疾病中使用氨基脲类化合物。特别地，本发明涉及一种治疗或预防受试者淀粉样相关疾病的方法，包括向受试者施用治疗剂量的氨基脲类化合物。根据本发明使用的化合物包括以下化学式的化合物，当施用时，可减少或抑制淀粉样纤维形成、神经退行性或细胞毒性：
• BACTERIAL EFFLUX PUMP INHIBITORS FOR THE TREATMENT OF OPHTHALMIC AND OTIC INFECTIONS
  申请人：Bostian Keith

  公开号：US20080132457A1

  公开（公告）日：2008-06-05

  Efflux pump inhibitors are co-administered with antimicrobial agents for the treatment of ophthalmic or otic infections. The agents may be co-administered directly to the site of infection (e.g., the eye or ear).

  流出泵抑制剂与抗微生物药物一起联合使用，用于治疗眼科或耳科感染。这些药物可以直接共同应用于感染部位（例如眼睛或耳朵）。
• US7947741B2
  申请人：——

  公开号：US7947741B2

  公开（公告）日：2011-05-24
• US7994225B2
  申请人：——

  公开号：US7994225B2

  公开（公告）日：2011-08-09
• Pentamidine Congeners. 2. 2-Butene-Bridged Aromatic Diamidines and Diimidazolines as Potential Anti-Pneumocystis carinii Pneumonia Agents
  作者：Isaac O. Donkor、Richard R. Tidwell、Susan K. Jones

  DOI：10.1021/jm00052a014

  日期：1994.12

  We have synthesized cis and trans geometric isomers 1-8 as semirigid congeners of pentamidine. Compounds 1-4 were more potent than pentamidine in treating Pneumocystis carinii pneumonia in immunosuppressed rats. These compounds also demonstrated no clinical toxicity or histopathologic abnormalities. Introduction of methoxy substituents meta to the amidine or imidazoline groups of the phenyl rings as in compounds 5-8 generally resulted in compounds with decreased anti-P. carinii activity and increased toxicity to the host. Compounds 1-4 were evaluated as DNA binders. These compounds showed greater affinity for poly(dA).poly(dT) than for calf thymus DNA. The cis isomers, 1 and 2, demonstrated greater affinity for DNA than their trans counterparts 3 and 4. This difference in DNA binding affinity, however, did not reflect in a corresponding difference in the anti-P. carinii activity of these compounds.