carbobenzyloxyglycinesuccinimido ester | 60341-62-0

• 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: carbobenzyloxyglycinesuccinimido ester
• 英文别名: Z-glycine-N-succinimidyl ester；Z-Gly-Succinimid
• CAS: 60341-62-0
• 化学式: C₁₄H₁₄N₂O₅
• 分子量: 290.276
• InChiKey: HCBWXZAHRLUELW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.59
• 重原子数：
  21.0
• 可旋转键数：
  4.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  92.78
• 氢给体数：
  1.0
• 氢受体数：
  5.0

反应信息

• 作为反应物：
  描述：

  carbobenzyloxyglycinesuccinimido ester 在 4-二甲氨基吡啶 、 sodium hydroxide 、 氨 、 臭氧 、 1-(3-二甲基氨基丙基)-3-乙基碳二亚胺 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 、 三乙胺 、 三氟乙酸 作用下， 以 甲醇 、 二氯甲烷 、 乙腈 、 xylene 为溶剂， 反应 6.0h， 生成 (R)-3-(Benzyloxycarbonylamino-methyl)-6-(tert-butyl-dimethyl-silanyloxy)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazole-1-carboxylic acid methyl ester
  参考文献：
  名称：

  Synthesis of a C₃-Symmetric Nanoscale Molecular Platform Based on Marine Cyclopeptides

  摘要：

  报道了一种高效合成构象预组织的三重对称分子平台的方法。该刚性骨架基于海洋环肽的结构，呈现出三个指向相同方向的功能团。双环咪唑构建模块从反式4-羟基-(S)-脯氨酸出发，经过七步合成得到。

  DOI：

  10.1055/s-2004-822906

文献信息

• The Synthesis and Inhibitory Activity of Dethiotrypanothione and Analogues against Trypanothione Reductase
  作者：Josephine A. Czechowicz、April K. Wilhelm、Maroya D. Spalding、Anna M. Larson、Linnea K. Engel、David G. Alberg

  DOI：10.1021/jo062597s

  日期：2007.5.1

  trypanosomatid parasite's defense against oxidative stress and has emerged as a promising target for antitrypanosomal drugs. We describe the synthesis and activity of dethiotrypanothione and analogues (2−4) as inhibitors of Trypanosoma cruzi TR. The syntheses of these macrocycles feature ring-closing olefin metathesis (RCM) reactions catalyzed by ruthenium catalyst 17. Derivative 4 is our most potent

  锥虫硫醚还原酶（TR）催化NADPH依赖性的锥虫硫醚二硫化物的还原（1）。TR在锥虫病寄生虫对氧化应激的防御中起着核心作用，并已成为抗锥虫病药物的有希望的靶标。我们描述了合成和dethiotrypanothione和类似物（活性2 - 4）作为抑制剂的克氏锥虫TR。这些大环的合成具有钌催化剂17催化的闭环烯烃复分解（RCM）反应。衍生物4是我们最有效的抑制剂，K i = 16μM。
• Mycrocycles useful in the teatment of Alzheimer's disease
  申请人：——

  公开号：US20030236199A1

  公开（公告）日：2003-12-25

  The present invention are macrocycles of the formula (IX): 1 for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

  本发明是一种用于治疗阿尔茨海默病和其他类似疾病的大环化合物（IX）的公式。这些化合物包括抑制β-分泌酶酶的抑制剂，对治疗阿尔茨海默病和其他以Aβ肽在哺乳动物体内沉积为特征的疾病有用。本发明的化合物在制药组合物和治疗方法中有用，可减少Aβ肽的形成。
• Synthesis, antibacterial activities, and pharmacological properties of enantiomers of temafloxacin hydrochloride
  作者：Daniel T. W. Chu、Carl W. Nordeen、Dwight J. Hardy、Robert N. Swanson、William J. Giardina、Andre G. Pernet、Jacob J. Plattner

  DOI：10.1021/jm00105a025

  日期：1991.1

  Temafloxacin hydrochloride [(+/-)-7-(3-methylpiperazin-1-yl)-6-fluro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride] is a potent member of the 4-pyridone-3-carboxylic acid class of antibacterial agents and is currently under clinical development as a broad-spectrum antimicrobial agent. It is a racemate having a chiral center at the C3 of the 7-piperazin-1-yl group. The two enantiomers were synthesized and tested for their antibacterial activities. Although no difference in in vitro antibacterial activities was observed, a minor difference in in vivo antibacterial activities was observed. However, they both exhibited similar pharmacological profiles.
• Fortimicin B cyclic carbamates
  作者：Jack Tadanier、Jerry R. Martin、Robert Hallas、Ronald Rasmussen、David Grampovnik、William Rosenbrook、William Arnold、Evelyn Schuber

  DOI：10.1016/s0008-6215(00)87137-2

  日期：1981.12