2-Guanidino-4,5-diphenyl-oxazol | 21324-58-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-Guanidino-4,5-diphenyl-oxazol
• 英文别名: (4,5-diphenyl-oxazol-2-yl)-guanidine；2-(4,5-Diphenyl-1,3-oxazol-2-yl)guanidine
• CAS: 21324-58-3
• 化学式: C₁₆H₁₄N₄O
• 分子量: 278.313
• InChiKey: RBYMBNRORJJIRO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  90.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (Z)-stilbenediol 、 二聚氰胺 在 盐酸 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 2-Guanidino-4,5-diphenyl-oxazol
  参考文献：
  名称：

  Loop,W. et al., Chemische Berichte, 1969, vol. 102, # 1, p. 230 - 242

  摘要：

  DOI：

文献信息

• Brain-specific drug delivery
  申请人：UNIVERSITY OF FLORIDA

  公开号：EP0218300A2

  公开（公告）日：1987-04-15

  The invention provides compounds adapted for the site-specific/sustained delivery of a centrally acting drug species to the brain having the formula [D-DHC] and the non- toxic pharmaceutically acceptable salts thereof, wherein [D] is a centrally acting drug species containing at least one reactive -OH, -COOH, -SH, -NH- or -NH2 functional group and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine ⇒ pyridinium salt redox carrier comprising a dihydroquinoline or dihydroisoquinoline ring system, a carbon atom of the nitrogen-containing ring portion of said ring system being connected via a bridging group to a reactive -OH, -COOH, -SH, -NH- or -NH2 functional group in the centrally acting drug species. The corresponding quaternary derivatives are also described.

  本发明提供了适用于向脑部定点/持续递送具有式[D-DHC]的中枢作用药物种类的化合物及其无毒药学上可接受的盐，其中[D]是含有至少一个活性-OH、-COOH、-SH、-NH-或-NH2官能团的中枢作用药物种类，[DHC]是还原的、可生物氧化的、二氢吡啶⇒吡啶鎓盐氧化还原载体的脂质形式，该载体包含二氢喹啉或二氢异喹啉环系统，所述环系统含氮环部分的碳原子通过桥基与中枢作用药物种类中的活性-OH、-COOH、-SH、-NH-或-NH2 官能团相连。还描述了相应的季衍生物。
• Pharmaceutical formulations for parenteral use
  申请人：UNIVERSITY OF FLORIDA

  公开号：EP0335545A2

  公开（公告）日：1989-10-04

  Aqueous parenteral solutions of drugs which are insoluble or only sparingly'soluble in water and/or which are unstable in water, combined with a hydroxypropyl,hydroxyethyl, glucosyl, maltosyl or maltotriosyl derivative of 3-or γ-cyclodextrin, provide a means for alleviating problems associated with drug precipitation at the injection site and/or in the lungs or other organs following parenteral administration.

  不溶于水或只能少量溶于水和/或在水中不稳定的药物的肠外水溶液与 3-或 γ-环糊精的羟丙基、羟乙基、葡糖基、麦芽糖基或麦芽三糖基衍生物结合使用，可以缓解肠外给药后药物在注射部位和/或肺部或其他器官沉淀的问题。
• Redox systems for brain-targeted drug delivery
  申请人：UNIVERSITY OF FLORIDA

  公开号：EP0327766A2

  公开（公告）日：1989-08-16

  Inclusion complexes of hydroxypropyl, hydroxyethyl, glucosyl, maltosyl or maltotriosyl derivatives of β- or γ-cyclodextrin with the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal forms of dihydropyridine = pyridinium salt redox systems for brain-targeted drug delivery provide a means for stabilizing the redox systems, particularly against oxidation. The redox inclusion complexes also provide a means for decreasing initial drug concentrations in the lungs after administration of the systems, leading to decreased toxicity. In selected instances, complexation results in substantially improved water solubility of the redox systems as well.

  β-或γ-环糊精的羟丙基、羟乙基、葡糖基、麦芽糖基或麦芽三糖基衍生物与还原型、可生物氧化、可穿透血脑屏障、类脂形式的二氢吡啶＝吡啶鎓盐氧化还原体系的包合物为脑靶向给药提供了一种稳定氧化还原体系，特别是防止氧化的方法。氧化还原包合物还能降低给药后肺部的初始药物浓度，从而降低毒性。在某些情况下，络合物还能大大提高氧化还原体系的水溶性。
• BRAIN-SPECIFIC DRUG DELIVERY
  申请人：UNIVERSITY OF FLORIDA

  公开号：EP0110955A1

  公开（公告）日：1984-06-20
• BRAIN-SPECIFIC ANALOGUES OF CENTRALLY ACTING AMINES
  申请人：UNIVERSITY OF FLORIDA

  公开号：EP0174342A1

  公开（公告）日：1986-03-19