2,4-bis(4-amidinophenyl)furan

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃
• 英文名称: 2,4-bis(4-amidinophenyl)furan
• 英文别名: DB690；3,5-Bis(4-amidinophenyl)furan；2,4-bis(4-guanylphenyl)furan；4-[4-(4-carbamimidoylphenyl)furan-2-yl]benzenecarboximidamide
• 化学式: C₁₈H₁₆N₄O
• 分子量: 304.351
• InChiKey: FUKWHJZCIGIYGP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  113
• 氢给体数：
  4
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  对氰基苯乙酮 在 盐酸 、 sodium hydroxide 、 trimethylsulfonium iodide 、 氨 、 溴 、 sodium hydride 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 、 氯仿 、 二甲基亚砜 为溶剂， 反应 157.5h， 生成 2,4-bis(4-amidinophenyl)furan
  参考文献：
  名称：

  2,4-Diphenyl Furan Diamidines as Novel Anti-Pneumocystis carinii Pneumonia Agents

  摘要：

  Dicationic 2,4-bis(4-amidinophenyl)furans 5-10 and 2,4-bis(4-amidinophenyl)-3,5-dimethylfurans 14 and 15 have been synthesized. Thermal melting studies revealed high binding affinity of the compounds to poly(dA-dT) and to the duplex oligomer d(CGCGAATTCGCG)(2). All of the new compounds were effective against Pneumocystis carinii pneumonia in the immunosuppressed rat model with up to 200-fold increase in activity compared to the control compound pentamidine. No toxicity was noted for 5, 7-10 at the dose of 10 mu mol/kg/d; however, the isopropyl analogue 7 showed toxicity comparable to pentamidine at the dosage of 20 mu mol/kg/d. Dimethylation of the parent compound on the furan ring resulted in reduced activity and increased toxicity.

  DOI：

  10.1021/jm990071c

文献信息

• Dicationic Compounds For Activity Against Trichomonas Vaginalis
  申请人：Boykin W. David

  公开号：US20070276020A1

  公开（公告）日：2007-11-29

  Dicationic compounds for the treatment of T. vaginalis infections are described. The presently described compounds exhibit in vitro activity against metronidazole-sensitive and -resistant T. vaginalis isolates. Furthermore, the presently described compounds demonstrate IC 50 concentrations that were not elevated in the metronidazole resistant isolate, suggesting that their activity is not affected by parasite mechanisms that confer resistance to 5-nitroimidizoles.

  本文描述了用于治疗T. vaginalis感染的二价化合物。目前描述的化合物在体外对甲硝唑敏感和耐药的T. vaginalis分离株具有活性。此外，目前描述的化合物表现出的IC50浓度在甲硝唑耐药分离株中没有升高，表明它们的活性不受寄生虫机制的影响，这些机制使其对5-硝基咪唑类药物产生耐药性。
• 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）。
• 2,4-Bis (4-amidino)phenyl furans as anti-pneumocystis carinii agents
  申请人：UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

  公开号：EP0941991B1

  公开（公告）日：2001-12-05
• 2,4-bis((4-Amidino)phenyl)furans as anti-pneumocystis carinii agents
  申请人：UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

  公开号：EP1130019B1

  公开（公告）日：2004-05-06