Boc-O-(2-bromo-Cbz)-L-Tyrosine

• 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: Boc-O-(2-bromo-Cbz)-L-Tyrosine
• 英文别名: 3-[4-[(2-bromophenyl)methoxycarbonyloxy]phenyl]-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoic acid
• 化学式: C₂₂H₂₄BrNO₇
• 分子量: 494.3
• InChiKey: UYWMYJQSTUVRHR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  31
• 可旋转键数：
  11
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  111
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  Boc-O-(2-bromo-Cbz)-L-Tyrosine 以60%的产率得到
  参考文献：
  名称：

  YAMASHIRO, DONALD, INT. J. PEPTIDE AND PROTEIN RES., 30,(1987) N 1, 9-12

  摘要：

  DOI：

文献信息

• Cholinergic Enhancers with Improved Blood-Brain Barrier permeability for the Treatment of Diseases Accompanied by Cognitive Impairment
  申请人：Maelicke Alfred

  公开号：US20080261954A1

  公开（公告）日：2008-10-23

  The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g. Galanthamine, narwedine and lycoramine, or from metabolites of said compounds.

  本发明涉及一种化合物，除了增强神经元胆碱能受体及外源性激动剂对乙酰胆碱和胆碱的敏感性，以及作为胆碱酯酶抑制剂和/或神经保护剂外，还具有比其母体化合物更强的血脑屏障通透性。这些化合物是从天仙子科生物碱（例如迎春花碱，纳威丁和莲花碱）或其代谢物中衍生出来的（可以通过其化学结构或直接通过化学合成来实现）。
• Fluorine containing atrial natriuretic peptides
  申请人：BIO-MEGA INC.

  公开号：EP0283956A2

  公开（公告）日：1988-09-28

  Disclosed herein are derivatives of atrial natriuretic peptides which are characterized by having (at positions 106 and/or 124) a phenylalanyl residue bearing a fluoro or trifluoromethyl substituent on the aromatic portion thereof. Optionally, the exocyclic N-terminal peptide segment and the first cystienyl residue (at position 105) are replaced by an optionally substituted thioalkanoyl residue. The derivatives possess useful diuretic, natriuretic and antihypertensive activities.

  本文公开了心房利钠肽的衍生物，其特征在于（在 106 和/或 124 位）苯丙氨酰残基在其芳香部分上带有氟或三氟甲基取代基。可选地，外环 N 端肽段和第一个胱氨酰残基（位于位置 105）被一个可选取代的硫代烷酰残基取代。这些衍生物具有有效的利尿、利尿和降压活性。
• Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment
  申请人：NEURODYN LIFE SCIENCES INC.

  公开号：US10265325B2

  公开（公告）日：2019-04-23

  A method for the treatment of a neurodegenerative, psychiatric or neurological disease associated with a cholinergic deficit comprising administering GLN-1062 or a pharmaceutically acceptable salt thereof by nasal administration to a patient in need thereof.

  一种治疗与胆碱能不足有关的神经退行性疾病、精神疾病或神经系统疾病的方法，包括通过鼻腔给药给有需要的患者施用 GLN-1062 或其药学上可接受的盐。