环(L-脯氨酰甘氨酰-L-脯氨酰甘氨酰-L-脯氨酰甘氨酰)

• 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
• 中文名称: 环(L-脯氨酰甘氨酰-L-脯氨酰甘氨酰-L-脯氨酰甘氨酰)
• 英文名称: Cyclo(-Pro-Gly)3
• 英文别名: (6S,15S,24S)-1,4,10,13,19,22-hexazatetracyclo[22.3.0.06,10.015,19]heptacosane-2,5,11,14,20,23-hexone
• 化学式: C₂₁H₃₀N₆O₆
• 分子量: 462.5
• InChiKey: WAOABPNIJIPSKM-KKUMJFAQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  33
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  148
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  Fmoc-L-脯氨酸 在 哌啶 、 (1-cyano-2-ethoxy-2-oxoethylidenaminooxy)dimethylaminomorpholinocarbenium hexafluorophosphate 、 N,N-二异丙基乙胺 、 2-肟氰乙酸乙酯 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 72.25h， 生成 环(L-脯氨酰甘氨酰-L-脯氨酰甘氨酰-L-脯氨酰甘氨酰)
  参考文献：
  名称：

  从含脯氨酸的环肽合成全肽基轮烷

  摘要：

  轮烷交联剂通过应力分散效应提高所得轮烷交联聚合物的韧性，这归因于互锁结构的流动性。迄今为止，轮烷交联剂的组成多样性受到限制，并且这些交联剂与肽和蛋白质的相容性差，这使得它们在此类材料中的使用具有挑战性。由肽组成的轮烷的合成可产生与肽和蛋白质相容的可生物降解交联剂，从而强化多肽和蛋白质，并最终导致具有优异机械性能和生物降解性的创新材料的开发。然而，由于肽中没有强结合基序，因此基于全肽的轮烷的化学合成仍然难以捉摸，这会阻止轴向肽穿透环肽。在这里，我们使用活性模板方法合成了全肽基轮烷，用于含脯氨酸的环肽。分子动力学模拟的结果表明，具有膨胀内腔和朝向中心的羰基氧的环状肽有利于轮烷合成。这种轮烷合成方法有望加速具有机械互锁结构的肽和蛋白质的合成，从而有可能开发具有前所未有的功能的肽基和蛋白质基材料。

  DOI：

  10.1021/acs.biomac.4c00257

文献信息

• Therapeutic agent composition and method of use, for treatment of mild congnitive impairment, depression, and psychological disorders
  申请人：Tran Lloyd Hung Loi

  公开号：US11090303B2

  公开（公告）日：2021-08-17

  The present invention generally relates to the use of cyclic Prolyl Glycine (“cyclic PG” or “cPG”) and analogues and mimetics thereof, as neuroprotective agents for the treatment and or prevention of cognitive impairment and neurological disorders including but not limited to cerebral ischemic or cerebral infarction, status epilepticus, perinatal asphyxia, anoxia, and cerebral trauma, as well as to the treatment and prevention of chronic neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease, and Huntington's disease, and as anticonvulsants. The present invention also generally provides manufacturing methods to prepare of dosage forms. The present invention further generally relates to the use of cyclic Prolyl Glycine and analogues and mimetics thereof, as neuroprotective and neuro-regenerating agents for the treatment and or prevention of depression and other psychological disorders.

  本发明一般涉及环脯氨酰甘氨酸（"环 PG "或 "cPG"）及其类似物和模拟物作为神经保护剂的用途，用于治疗和或预防认知障碍和神经系统疾病，包括但不限于脑缺血或脑梗塞、癫痫状态、围产期窒息、缺氧和脑外伤，以及治疗和预防慢性神经退行性疾病，如阿尔茨海默氏症、状态性癫痫、围产期窒息、缺氧和脑外伤，以及治疗和预防阿尔茨海默病、帕金森病和亨廷顿病等慢性神经退行性疾病，并用作抗惊厥药。本发明一般还提供制备剂型的生产方法。本发明一般还涉及环脯氨酰甘氨酸及其类似物和模拟物作为神经保护剂和神经再生剂用于治疗和或预防抑郁症及其他心理疾病的用途。
• THERAPEUTIC AGENT COMPOSITION AND METHOD OF USE, FOR TREATMENT OF MILD CONGNITIVE IMPAIRMENT, DEPRESSION, AND PSYCHOLOGICAL DISORDERS
  申请人：Tran Lloyd Hung Loi

  公开号：US20200054629A1

  公开（公告）日：2020-02-20

  The present invention generally relates to the use of cyclic Prolyl Glycine (“cyclic PG” or “cPG”) and analogues and mimetics thereof, as neuroprotective agents for the treatment and or prevention of cognitive impairment and neurological disorders including but not limited to cerebral ischemic or cerebral infarction, status epilepticus, perinatal asphyxia, anoxia, and cerebral trauma, as well as to the treatment and prevention of chronic neurodegenerative disorders such as Alzheimer's disease, Parkinson's disease, and Huntington's disease, and as anticonvulsants. The present invention also generally provides manufacturing methods to prepare of dosage forms. The present invention further generally relates to the use of cyclic Prolyl Glycine and analogues and mimetics thereof, as neuroprotective and neuro-regenerating agents for the treatment and or prevention of depression and other psychological disorders.