(2S)-2-acetamido-4-(1H-indol-3-yl)butanoic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (2S)-2-acetamido-4-(1H-indol-3-yl)butanoic acid
• 化学式: C₁₄H₁₆N₂O₃
• 分子量: 260.29
• InChiKey: TZVGIHUGMJIKMD-ZDUSSCGKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  82.2
• 氢给体数：
  3
• 氢受体数：
  3

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.

  本发明提供一种改性乳铁蛋白肽，其具有细胞毒性，长度为7至25个氨基酸，含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氨基酸，以及其酯、酰胺、盐和环状衍生物，以及制备这些肽的方法、含有这些肽的药物组合物和将这些肽用作药物的用途，特别是作为抗菌或抗肿瘤剂。
• Antimicrobial compounds and formulations
  申请人：——

  公开号：US20030195144A1

  公开（公告）日：2003-10-16

  The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipoophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilising microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

  本发明涉及使用分子制造药物，该分子包括长度为2至35个非氢原子的骨架，至少连接有两个笨重和亲脂性基团，并且具有至少一个阳离子多于阴离子的基团，用作破坏微生物细胞膜的药物，并且涉及使用包括长度为2至35个非氢原子的骨架的分子，该分子共价连接有一个超级笨重和亲脂性基团，包括至少9个非氢原子，并且具有至少两个阳离子多于阴离子的基团，作为膜作用抗微生物药物的用途，以及涉及此类分子的治疗方法，特别是包括肽衍生物和肽类似物的肽。
• 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。
• Antimicrobial Compounds and Formulations
  申请人：Svendsen John Sigurd

  公开号：US20120108520A1

  公开（公告）日：2012-05-03

  The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilising microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

  本发明涉及使用一种分子，其包含长度为2至35个非氢原子的骨架，并且至少连接有两个笨重和亲脂性基团，并且具有至少一个阳离子大于阴离子的基团，在制造破坏微生物细胞膜的药物方面使用该分子。另外，本发明还涉及使用一种分子作为膜作用抗微生物剂，该分子包括长度为2至35个非氢原子的骨架，并且共价连接有一个超大的、亲脂性的基团，包括至少9个非氢原子，并且具有至少两个阳离子大于阴离子的基团。本发明还涉及涉及这样的分子的治疗方法，特别是包括肽衍生物和肽类似物的肽。
• 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。