N^α-i-Butyl-N^β-Fmoc hydrazine

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: N^α-i-Butyl-N^β-Fmoc hydrazine
• 英文别名: N'-2-isobutyl-fluorenylmethyl carbazate；N-fluorenylmethyloxycarbonyl-N'-(2-methylpropyl) hydrazine；Fmoc-aza-Leu；9H-fluoren-9-ylmethyl N-(2-methylpropylamino)carbamate
• 化学式: C₁₉H₂₂N₂O₂
• 分子量: 310.396
• InChiKey: IROJPMDSSMWDCF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  50.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N^α-i-Butyl-N^β-Fmoc hydrazine 在 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 3.0h， 生成 His-D-Trp-AzaLeu-Trp-D-Phe-NH2
  参考文献：
  名称：

  Azapeptide Analogues of the Growth Hormone Releasing Peptide 6 as Cluster of Differentiation 36 Receptor Ligands with Reduced Affinity for the Growth Hormone Secretagogue Receptor 1a

  摘要：

  The synthetic hexapeptide growth hormone releasing peptide-6 (GHRP-6) exhibits dual affinity for the growth hormone secretagogue receptor la (GHS-R1a) and the cluster of differentiation 36 (CD36) receptor. Azapeptide GHRP-6 analogues have been synthesized, exhibiting micromolar affinity to the CD36 receptor with reduced affinity toward the GHS-R1a. A combinatorial split-and-mix approach furnished aza-GHRP-6 leads, which were further examined by alanine scanning. Incorporation of an aza-amino acid residue respectively at the D-Trp(2) Ala(3), or Trp(4) position gave aza-GHRP-6 analogues with reduced affinity toward the GHS-R1a by at least a factor of 100 and in certain cases retained affinity for the CD36 receptor. In the latter cases, the D-Trp2 residue proved important for CD36 receptor affinity; however, His' could be replaced by Ala' without considerable loss of binding. In a microvascular sprouting assay using a choroid explant, [azaTyr(4)]-GHRP-6 (15), [Ala(1), azaPhe(2)]-GHRP-6 (16), and [azaLeu(3), Ala(6)]-GHRP-6 (33) all exhibited antiangiogenic activity.

  DOI：

  10.1021/jm300557t
• 作为产物：
  描述：

  9-芴基甲基肼基甲酸酯 在 盐酸 、 sodium cyanoborohydride 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 16.5h， 生成 N^α-i-Butyl-N^β-Fmoc hydrazine
  参考文献：
  名称：

  Stable peptide-based PACE4 inhibitors

  摘要：

  提供了PACE4抑制剂及其用于治疗感染和癌症的用途。特别地，提供了一种方法或用于治疗受试者癌症的用途，包括向受试者施用PACE4抑制剂或所披露的组合物的治疗有效量。

  公开号：

  US09809621B2

文献信息

• Stable peptide-based PACE4 inhibitors
  申请人：Day Robert

  公开号：US09809621B2

  公开（公告）日：2017-11-07

  It is provided PACE4 inhibitors and their uses for treating infection, cancer. Particularly, it is provided a method or use for the treatment of a cancer in a subject, comprising administering to the subject a therapeutically effective amount of the PACE4 inhibitors or the composition disclosed.

  提供了PACE4抑制剂及其用于治疗感染和癌症的用途。特别地，提供了一种方法或用于治疗受试者癌症的用途，包括向受试者施用PACE4抑制剂或所披露的组合物的治疗有效量。
• [EN] PEPTIDE ANTIBIOTICS<br/>[FR] ANTIBIOTIQUES PEPTIDIQUES
  申请人：UNIV QUEENSLAND

  公开号：WO2019084628A1

  公开（公告）日：2019-05-09

  There is provided a range of novel compounds. These novel compounds may demonstrate a broad spectrum antibacterial and antifungal activity. These compounds may be active against the emerging polymyxin resistant bacteria. These compounds may also be useful when used in conjunction with other pharmaceutically active agents.

  提供了一系列新化合物。这些新化合物可能表现出广谱抗菌和抗真菌活性。这些化合物可能对新出现的多粘菌素耐药细菌具有活性。这些化合物在与其他药用活性剂一起使用时也可能很有用。
• Aza-amino acid scanning of chromobox homolog 7 (CBX7) ligands
  作者：Mariam Traoré、Michael Gignac、Ngoc-Duc Doan、Fraser Hof、William D. Lubell

  DOI：10.1002/psc.2982

  日期：2017.4

  An aza‐amino acid scan of peptide inhibitors of the chromobox homolog 7 (CBX7) was performed to study the conformational requirements for affinity to the methyllysine reader protein. Twelve azapeptide analogues were prepared using three different approaches employing respectively N‐(Fmoc)aza‐amino acid chlorides and submonomer azapeptide synthesis to install systematically aza‐residues at the first

  对色谱盒同系物7（CBX7）的肽抑制剂进行了氮杂氨基酸扫描，以研究其对甲基赖氨酸阅读器蛋白亲和力的构象要求。使用三种不同的方法制备了十二种氮杂肽类似物，分别采用N-（Fmoc）氮杂氨基酸氯化物和亚单体氮杂肽合成方法，在肽的前四个残基上系统地安装氮杂残基，并提供具有饱和和不饱和侧链。在色谱盒同系物7结合试验中评估了氮杂肽配体，为深入了解亲和力的结构要求提供了有用的信息。版权所有©2017欧洲多肽协会和John Wiley＆Sons，Ltd.
• STABLE PEPTIDE-BASED FURIN INHIBITORS
  申请人：Day Robert

  公开号：US20150141324A1

  公开（公告）日：2015-05-21

  It is provided furin inhibitors and their uses for treating pathogen infection. Particularly, it is provided a method or use for the treatment of a pathogen infection, in a subject, comprising administering to the subject a therapeutically effective amount of the furin inhibitors or the composition disclosed, thereby preventing or treating pathogen infection, in the subject.

  本发明提供了抑制酶furin及其用于治疗病原体感染的方法。特别地，本发明提供了一种治疗主体的病原体感染的方法或用途，包括向该主体投予治疗有效量的furin抑制剂或所披露的组合物，从而预防或治疗该主体的病原体感染。
• STABLE PEPTIDE-BASED PACE4 INHIBITORS
  申请人：Day Robert

  公开号：US20140206622A1

  公开（公告）日：2014-07-24

  It is provided PACE4 inhibitors and their uses for treating infection, cancer. Particularly, it is provided a method or use for the treatment of a cancer in a subject, comprising administering to the subject a therapeutically effective amount of the PACE4 inhibitors or the composition disclosed.

  本文提供了PACE4抑制剂及其用于治疗感染和癌症的方法。特别地，本文提供了一种用于治疗患者癌症的方法或用途，包括向患者施用足够治疗量的PACE4抑制剂或所述的组合物。