glycyl=>glycyl=>L-aspartic acid ; N-(N-glycyl-glycyl)-L-aspartic acid | 142214-60-6

• 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: glycyl=>glycyl=>L-aspartic acid ; N-(N-glycyl-glycyl)-L-aspartic acid
• 英文别名: N-(N-Glycyl-glycyl)-L-asparaginsaeure；L-[(Aminoacetyl-amino)-acetamino]-bernsteinsaeure；Glycyl=>glycyl=>L-asparaginsaeure; N-(N-Glycyl-glycyl)-L-asparaginsaeure；Gly-Gly-Asp；(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]butanedioic acid
• CAS: 142214-60-6
• 化学式: C₈H₁₃N₃O₆
• 分子量: 247.208
• InChiKey: UFPXDFOYHVEIPI-BYPYZUCNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -5.2
• 重原子数：
  17
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  159
• 氢给体数：
  5
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  甘氨酰-L-天冬氨酸 、 氯乙酰氯 在 sodium hydroxide 作用下， 生成 glycyl=>glycyl=>L-aspartic acid ; N-(N-glycyl-glycyl)-L-aspartic acid
  参考文献：
  名称：

  Suzuki, Journal of Biochemistry, 1931, vol. 13, p. 57,70

  摘要：

  DOI：

文献信息

• SOLOMONAMIDE ANALOGUE COMPOUNDS, PHARMACEUTICALS CONTAINING SOLOMONAMIDE ANALOGUE COMPOUNDS, AND PROCESSES FOR THE PREPARATION THEREOF
  申请人：COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH

  公开号：US20150291659A1

  公开（公告）日：2015-10-15

  Solomanamide analogues of Formula-I having anti-inflammatory activity, and viable synthetic routes for the preparation of such analogues, including the synthesis of macrocyclic core of Salomanamide analogues. The Solomanamide analogues of Formula-I or their pharmaceutical salt may be provided in a pharmaceutical composition and administered in an effective amount for the treatment of inflammation and/or pain.

  公式I的Solomanamide类似物具有抗炎活性，并且具有制备这种类似物的可行合成路线，包括制备Salomanamide类似物的大环核心的合成。公式I的Solomanamide类似物或其药物盐可以在药物组合物中提供，并以有效剂量用于治疗炎症和/或疼痛。
• Radiolabeled technetium chelates for use in renal function determinations
  申请人：UNIVERSITY OF UTAH RESEARCH FOUNDATION

  公开号：EP0173424A1

  公开（公告）日：1986-03-05

  The present invention is directed to novel radiopharmaceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: wherein X is S or N; and wherein Y is -H2 or wherein Y is and where R, is -H, -CH3, or -CH2CH3; R2 is -H, -CH2CO2H, -CH2CONH2, -CH2CH2C02H, -CH2CH2CONH2, -CH3, -CH2CH3, CH2C6H5, or -CH20H; and Z is -H, -CO2H, -CONH2, -S03H, -SO2NH2, or -CONHCH2C02H; and the Tc is Tc-99m; and water-soluble salts thereof. Of the foregoing, the presently preferred Tc-99m compound of the present invention is Tc-99m-mercaptoacetylglycylglycylglycine (Tc-99m-MAGGG). The present invention is also directed to novel chelating agents that may be reacted with Tc-99m to form the foregoing compounds. Such novel chelating agents have the following general formula. where X and Y have the same definitions as above, and wherein Y' is -H2 when X is N, or wherein Y' is -H, or a suitable protective group such as -COCH3, -COC6H5, -CH2NHCOCH3, -COCF3, or -COCH20H when X is S. The present invention also provides methods for preparing and using the novel Tc-99m compounds.

  本发明涉及以 Tc-99m 为放射性标记的新型放射性药物成像剂。特别是，本发明公开的新型成像剂具有相对较高的肾提取效率，因此可用于进行肾功能成像程序。本发明的新型 Tc-99m 化合物具有以下通式： 其中 X 是 S 或 N；Y 是 -H2 或 Y 是 其中 R 是-H、-CH3 或-CH2CH3；R2 是-H、-CH2CO2H、-CH2CONH2、-CH2CH2C02H、-CH2CH2CONH2、-CH3、-CH2CH3、CH2C6H5 或-CH20H；Z是-H、-CO2H、-CONH2、-S03H、-SO2NH2或-CONHCH2C02H；Tc是Tc-99m；以及它们的水溶性盐。在上述化合物中，本发明目前优选的 Tc-99m 化合物是 Tc-99m-巯基乙酰甘氨酰甘氨酸（Tc-99m-MAGGG）。本发明还涉及可与 Tc-99m 反应生成上述化合物的新型螯合剂。此类新型螯合剂具有以下通式。 其中 X 和 Y 的定义同上，当 X 为 N 时，Y'为-H2；当 X 为 S 时，Y'为-H 或合适的保护基团，如-COCH3、-COC6H5、-CH2NHCOCH3、-COCF3 或-COCH20H。 本发明还提供了制备和使用新型 Tc-99m 化合物的方法。
• A PROCESS FOR THE PREPARATION OF SOLOMONAMIDE ANALOGUES
  申请人：Council of Scientific & Industrial Research

  公开号：EP2925771A1

  公开（公告）日：2015-10-07
• US4980147A
  申请人：——

  公开号：US4980147A

  公开（公告）日：1990-12-25
• US5322929A
  申请人：——

  公开号：US5322929A

  公开（公告）日：1994-06-21