Bz(4-OH)-D-Leu-D-Val-D-Phe-D-Phe-D-Ala-NH2

• 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: Bz(4-OH)-D-Leu-D-Val-D-Phe-D-Phe-D-Ala-NH2
• 英文别名: N-[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-amino-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]-4-hydroxybenzamide
• 化学式: C₃₉H₅₀N₆O₇
• 分子量: 714.8
• InChiKey: GXQQVKVHKBLOPI-AQZGVYKSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  52
• 可旋转键数：
  18
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  209
• 氢给体数：
  7
• 氢受体数：
  7

文献信息

• Modulators of beta-amyloid peptide aggregation comprising D-amino acids
  申请人：Praecis Pharmaceuticals Incorporated

  公开号：EP1586584A1

  公开（公告）日：2005-10-19

  Compounds that medlate natural β-amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β-amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-viline. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a β-amyloid peptide, preferably a retro-inverso isomer of Aβ17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amylaidogenic diseases using the compounds of the invention, are also disclosed.

  本发明提供了可调解天然β-淀粉样肽聚集的化合物。本发明的调节剂包括一种完全由 D-氨基酸组成的肽，最好是基于 β-淀粉样肽的肽。优选地，该肽由 3-5 个 D-氨基酸残基组成，并包括至少两个独立选自 D-亮氨酸、D-苯丙氨酸和 D-丝氨酸组成的组的 D-氨基酸残基。在一个特别优选的实施方案中，多肽是β-淀粉样肽的逆反异构体，最好是Aβ17-21的逆反异构体。在某些实施方案中，肽的氨基末端、羧基末端或氨基末端和羧基末端均被修饰。优选的氨基末端修饰基团包括环基、杂环基、多环基和支链烷基。优选的羧基末端修饰基团包括酰胺基、烷基酰胺基、芳基酰胺基或羟基。此外，还公开了包含本发明化合物的药物组合物，以及使用本发明化合物诊断和治疗淀粉样变性疾病的方法。
• Methods for enhancing the bioavailability of a drug
  申请人：Hayward J. Neil

  公开号：US20050288222A1

  公开（公告）日：2005-12-29

  The invention provides methods and compositions for enhancing the bioavailability of a drug in a subject. The present invention also provides methods and compositions for treating or preventing hepatic injury in a subject in need thereof. The invention further provides methods for identifying hydrophobic peptides, e.g., β-amyloid peptide derivatives, which are useful in enhancing bioavailability of a drug in a subject.

  本发明提供了提高药物在受试者体内的生物利用度的方法和组合物。本发明还提供了在有需要的受试者中治疗或预防肝损伤的方法和组合物。本发明进一步提供了鉴定疏水肽，例如β-淀粉样蛋白肽衍生物的方法，这些疏水肽有助于提高药物在受试者体内的生物利用度。
• MODULATORS OF beta-AMYLOID PEPTIDE AGGREGATION COMPRISING D-AMINO ACIDS
  申请人：Praecis Pharmaceuticals Incorporated

  公开号：EP0929574B1

  公开（公告）日：2005-06-29
• US6277826B1
  申请人：——

  公开号：US6277826B1

  公开（公告）日：2001-08-21
• US6689752B2
  申请人：——

  公开号：US6689752B2

  公开（公告）日：2004-02-10