bis(N-(2-phenylethyl)guanidine); sulfuric acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机硫酸及其衍生物
• 英文名称: bis(N-(2-phenylethyl)guanidine); sulfuric acid
• 英文别名: 2-(2-phenylethyl)guanidine;sulfuric acid
• 化学式: C18H28N6O4S
• 分子量: 424.5
• InChiKey: KXSOPULWBBJOOF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.35
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  212
• 氢给体数：
  6
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-苯乙胺 、 S-甲基异硫脲硫酸盐 在 水 、 丙酮 、 乙醚 作用下， 以 乙醇 为溶剂， 反应 5.0h， 以The reaction yielded 61.5% (9.14 g) 2-phenylethylguanidine hemisulfate的产率得到bis(N-(2-phenylethyl)guanidine); sulfuric acid
  参考文献：
  名称：

  Inhibition of tumour growth

  摘要：

  本发明提供了一种具有三个或更多阳离子残基的细胞毒性7到25个氨基酸肽，其中具有一个或多个非遗传性的大体积和亲脂性氨基酸，以及它们的酯、酰胺、盐和环状衍生物的制备方法，含有它们的制药组合物以及它们作为药物的使用，特别是作为抗菌或抗肿瘤剂。在一个优选方面，本发明提供了使用所述肽在诱导受体中的肿瘤生长或建立的适应性免疫方法，以及使用其他裂解剂在受体中诱导适应性免疫的方法。

  公开号：

  US08283315B2

文献信息

• Bioactive peptides
  申请人：ALPHARMA AS

  公开号：US20030022821A1

  公开（公告）日：2003-01-30

  The present invention provides a modified lactoferrin peptide which is cytotoxic, 7 to 25 amino acids in length, with three or more cationic residues and which has one or more extra bulky and lipophilic amino acids as compared to the native lactoferrin sequence, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing such peptides, pharmaceutical compositions containing such peptides and use of the peptides as medicaments, particularly as antibacterials or anti-tumoural agents.

  本发明提供了一种改良的乳铁蛋白肽，具有细胞毒性，长度为7至25个氨基酸，具有三个或更多阳离子残基，并且与天然乳铁蛋白序列相比，具有一个或多个额外的笨重和亲脂性氨基酸，以及其酯类，酰胺，盐和环状衍生物，以及制备这种肽的方法，包含这种肽的药物组合物以及将这种肽用作药物，特别是用作抗菌或抗肿瘤剂。
• Cytotoxic modified lactoferrin peptides
  申请人：Svendsen John Sigurd

  公开号：US06890902B2

  公开（公告）日：2005-05-10

  The present invention provides a modified lactoferrin peptide which is cytotoxic, 7 to 25 amino acids in length, with three or more cationic residues and which has one or more extra bulky and lipophilic amino acids as compared to the native lactoferrin sequence, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing such peptides, pharmaceutical compositions containing such peptides and use of the peptides as medicaments, particularly as antibacterials or anti-tumoural agents.

  本发明提供了一种改良的乳铁蛋白肽，其具有细胞毒性，长度为7至25个氨基酸，具有三个或更多阳离子残基，并且与天然乳铁蛋白序列相比，具有一个或多个额外的笨重和亲脂性氨基酸，以及其酯类、酰胺、盐和环状衍生物，以及制备这种肽的方法，含有这种肽的药物组合物和将这种肽用作药物，特别是作为抗菌或抗肿瘤剂。
• Inhibition of tumour growth
  申请人：Eliassen Tone Liv

  公开号：US20080019993A1

  公开（公告）日：2008-01-24

  The present invention provides a cytotoxic 7 to 25 mer peptide with three or more cationic residues which has one or more non-genetic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them and their use as medicaments, particularly as antibacterions or antitumoural agents. In a preferred aspect, the invention provides the use of said peptides in a method of inducing adaptive immunity against tumour growth or establishment in a subject, as well as the use of other lytic agents in a method of inducing adaptive immunity in a subject.

  本发明提供了一种细胞毒性的7至25个氨基酸残基的肽，其中含有三个或更多阳离子残基，其中含有一个或多个非遗传性的臃肿和亲脂性氨基酸，以及它们的酯类、酰胺、盐和环状衍生物，以及制备这些肽的方法、含有它们的药物组合物以及它们作为药物的用途，特别是作为抗菌或抗肿瘤剂。在一个优选方面，本发明提供了利用所述肽在主体中诱导适应性免疫反应以抑制肿瘤生长或建立的方法，以及利用其他溶解剂在主体中诱导适应性免疫反应的方法。
• INHIBITION OF TUMOR GROWTH
  申请人：Eliassen Liv Tone

  公开号：US20140037657A1

  公开（公告）日：2014-02-06

  The present invention provides a cytotoxic 7 to 25 mer peptide with three or more cationic residues which has one or more non-genetic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them and their use as medicaments, particularly as antibacterions or antitumoral agents. In a preferred aspect, the invention provides the use of said peptides in a method of inducing adaptive immunity against tumor growth or establishment in a subject, as well as the use of other lytic agents in a method of inducing adaptive immunity in a subject.

  本发明提供了一种具有三个或更多阳离子残基的细胞毒性7到25个氨基酸肽，其中具有一个或多个非遗传性臃肿和亲脂氨基酸，以及它们的酯，酰胺，盐和环状衍生物，以及制备肽的方法，含有它们的制药组合物以及它们作为药物的用途，特别是作为抗菌或抗肿瘤剂。在一个优选方面，本发明提供了在诱导受体中适应性免疫反应以抑制肿瘤生长或建立的方法中使用所述肽的用途，以及在诱导受体中适应性免疫反应的方法中使用其他溶解剂的用途。
• Inhibition of tumor growth
  申请人：Eliassen Liv Tone

  公开号：US09109048B2

  公开（公告）日：2015-08-18

  The present invention provides a cytotoxic 7 to 25 mer peptide with three or more cationic residues which has one or more non-genetic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them and their use as medicaments, particularly as antibacterions or antitumoral agents. In a preferred aspect, the invention provides the use of said peptides in a method of inducing adaptive immunity against tumor growth or establishment in a subject, as well as the use of other lytic agents in a method of inducing adaptive immunity in a subject.

  本发明提供了一种细胞毒性的7到25个氨基酸残基的肽，其中有三个或更多阳离子残基，其中包含一个或多个非遗传性的体积庞大和亲脂性的氨基酸，以及它们的酯、酰胺、盐和环状衍生物，以及制备这些肽的方法、含有它们的制药组合物以及它们作为药物的用途，特别是作为抗菌或抗肿瘤剂。在一个优选方面，本发明提供了使用所述肽在受体中诱导适应性免疫反应来抵抗肿瘤生长或建立的方法，以及使用其他溶解剂在受体中诱导适应性免疫反应的方法。