Mva-Leu-OH

• 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: Mva-Leu-OH
• 英文别名: (2S)-4-methyl-2-(4-methylpentanoylamino)pentanoic acid
• 化学式: C₁₂H₂₃NO₃
• 分子量: 229.32
• InChiKey: LDKRDUZVXNEFNX-JTQLQIEISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  16
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Mva-Leu-OH 、 在 N-甲基吗啉 、 1-羟基苯并三唑 、 N,N'-二环己基碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 7.0h， 以43%的产率得到Mva-Leu-Azy-OBzl
  参考文献：
  名称：

  On the synthesis of (2S)-aziridine-2-carboxylic acid containing peptides

  摘要：

  Optimized conditions are described for the synthesis of 1-trityl-2-aziridine-carboxylic acid 3 (Trt-Azy-OH) and benzyl (2S)-aziridine-2-carboxylate 6 (H-Azy-OBzl) as useful derivatives for the synthesis of N- and C-terminal aziridine-containing peptides. Thereby, the use of the pentafluorophenyl ester of Trt-Azy-OH was found to be the method of choice in acylating steps, whereas acylation of H-Azy-OBzl several classical methods of peptide synthesis can be successfully used. The fully protected aziridine-2-carboxylic acid peptides are accessible in satisfactory yields as analytically defined products, but partial or total deprotection of these compounds again by standard procedures of peptide synthesis is surprisingly difficult in terms of satisfactory yields, whereby sequence-dependent unstability both in the reaction and purification steps as well as on storage was found to strongly limit the accessibility of these aziridine-containing peptides as promising active-site inactivators of cysteine-proteinases.

  DOI：

  10.1016/s0040-4020(01)80847-4
• 作为产物：
  描述：

  L-亮氨酸 、 4-甲基戊酸 在 adenosine monophosphate ligase SfaB from Streptomyces thioluteus 、 5’-三磷酸腺苷 、 magnesium chloride 、 Cleland's reagent 作用下， 以 aq. buffer 为溶剂， 反应 6.0h， 生成 Mva-Leu-OH
  参考文献：
  名称：

  重新利用3-异氰基丁酸腺苷酸化酶SfaB进行多功能酰胺化和硫酯化

  摘要：

  微生物天然产物的基因组挖掘使化学家不仅能够发现具有新颖骨架的生物活性分子，而且能够识别催化多种化学反应的酶。探索这些生物合成酶的底物混杂性和催化机理有助于开发潜在的生物催化剂。SfaB是一种形成酰基腺苷酸的酶，可在由硫链霉菌产生的二异腈自然产物SF2768的生物合成途径中，对独特的结构单元3-异氰基丁酸进行腺苷酸化。，并且该AMP连接酶被证明可以接受各种短链脂肪酸（SCFA）。在本文中，我们将SfaB重新用于催化那些SCFA与各种胺或硫醇亲核试剂之间的酰胺化或硫酯化反应，从而提供了另一种酶促方法来体外制备相应的酰胺和硫酯。

  DOI：

  10.1002/anie.202010042

文献信息

• NOVEL ANTI-DIABETIC PEPTIDES
  申请人：AMYLIN PHARMACEUTICALS, INC.

  公开号：EP1104438A2

  公开（公告）日：2001-06-06
• US6087334A
  申请人：——

  公开号：US6087334A

  公开（公告）日：2000-07-11
• [EN] NOVEL ANTI-DIABETIC PEPTIDES<br/>[FR] NOUVEAUX PEPTIDES ANTIDIABETIQUES
  申请人：AMYLIN PHARMACEUTICALS INC

  公开号：WO2000011029A2

  公开（公告）日：2000-03-02

  Compounds of formula (I) which act as amylin agonists with respect to certain desired amylin activities and as calcitonin agonists with respect to certain desired calcitonin activities are provided. Such compounds are useful in treating disturbances in fuel metabolism in mammals, including, but not limited to diabetes mellitus, including Type I diabetes and Type II diabetes. The present invention also relates to methods of treating Type I diabetes, treating Type II diabetes and to methods of beneficially regulating gastrointestinal motility comprising administration of a therapeutically effective amount of one of the compounds. Also provided are pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier.