Z-Lys-ONPh | 23370-97-0

• 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: Z-Lys-ONPh
• 英文别名: p-Nitrophenylester von N^α-Z-Lysin；N-A-Cbz-L-lysinep-nitrophenylester；(4-nitrophenyl) 6-amino-2-(phenylmethoxycarbonylamino)hexanoate
• CAS: 23370-97-0
• 化学式: C₂₀H₂₃N₃O₆
• 分子量: 401.419
• InChiKey: VMKGUOYDQYWEJP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  29
• 可旋转键数：
  11
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  137
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• DIPEPTIDE MIMETICS OF NGF AND BDNF NEUROTROPHINS
  申请人：Seredenin Sergey Borisovich

  公开号：US20110312895A1

  公开（公告）日：2011-12-22

  The invention relates to compounds having either agonist or antagonist activities for the neurotrophins NGF and BDNF and represented by monomeric or dimeric substituted dipeptides that are analogs of the exposed portions of loop 1 or loop 4 regions of these neurotrophins near or at a beta-turn of the respective loop. N-acylated substituents of these dipeptides are biostereoisomers of the amino acid residues preceding these dipeptide sequences in the neurotrophin primary structure. The dimeric structure is produced advantageously by using hexamethylenediamine to which dipeptides are attached via their carboxyl groups. The claimed compounds displayed neuroprotective and differentiation-inducing activities in cellular models and enhanced the amount of phosphorylated tyrosine kinase A and the heat shock proteins Hsp32 and Hsp70 in the concentration range of 10 −9 to 10 −5 M. They also displayed neuroprotective, anti-parkinsonian, anti-stroke, anti-ischemic, anti-depressant and anti-amnestic activities in animal models and were active in experimental models of Alzheimer's disease. These in vivo effects of the claimed compounds are displayed in the dose range of 0.01 to 10 mg/kg when administered intraperitoneally.

  该发明涉及具有神经营养因子NGF和BDNF的激动剂或拮抗剂活性的化合物，这些化合物由单体或二聚体取代二肽代表，这些二肽代表这些神经营养因子的环1或环4区域的暴露部分的类似物，靠近或在各自环的β-转弯处。这些二肽的N-酰化取代物是神经营养因子原始结构中这些二肽序列之前的氨基酸残基的生物立体异构体。通过使用己二胺，优点地产生二聚体结构，二肽通过它们的羧基团连接到己二胺上。所述化合物在细胞模型中显示出神经保护和诱导分化活性，并在浓度范围为10^(-9)到10^(-5)M时增加了磷酸化酪氨酸激酶A和热休克蛋白Hsp32和Hsp70的量。它们还在动物模型中显示出神经保护、抗帕金森病、抗中风、抗缺血、抗抑郁和抗遗忘活性，并在阿尔茨海默病的实验模型中活跃。所述化合物的这些体内效应在腹腔内给药时的剂量范围为0.01至10毫克/千克。
• US9683014B2
  申请人：——

  公开号：US9683014B2

  公开（公告）日：2017-06-20