L-丙氨酸4-硝基酰苯胺 | 1668-13-9

• 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: L-丙氨酸4-硝基酰苯胺
• 英文名称: L-alanine-p-nitroanilide
• 英文别名: Alanine-4-nitroanilide；L-alanine para-nitroanilide；L-alanine p-nitroanilide；alanine p-nitroanilide；alanine-p-nitroanilide；L-Ala-p-nitroanilide；L-Alanine-4-nitroanilide；(2S)-2-amino-N-(4-nitrophenyl)propanamide
• CAS: 1668-13-9
• 化学式: C₉H₁₁N₃O₃
• mdl: MFCD06810060
• 分子量: 209.205
• InChiKey: PXFUDSMGEYRNNC-LURJTMIESA-N

物化性质

• 熔点：
  95 °C
• 沸点：
  443.4±30.0 °C(Predicted)
• 密度：
  1.350±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 储存条件：
  -15°C下密封储存

反应信息

• 作为反应物：
  描述：

  L-丙氨酸4-硝基酰苯胺 在 水 作用下， 以 丙酮 为溶剂， 生成 4-硝基苯胺
  参考文献：
  名称：

  Polarographic study of hydrolysis of [8-lysine]vasopressin and its derivatives with blood serum of pregnant women

  摘要：

  对孕妇血清中[8-赖氨酸]加压素及一些加压素类激素的水解进行了极谱研究。研究了水解对pH的依赖性（pH最适值：7.4-7.50，底物浓度（Km 1.2 . 10^-5M），pH稳定性和热稳定性。各个加压素类似物的水解速率按顺序递减：[8-赖氨酸]加压素 > Nα-甘氨酰-脯氨酰[8-赖氨酸]-加压素 > Nα-亮氨酰-[8-赖氨酸]加压素 > Nα-丙氨酰-[8-赖氨酸]加压素 > Nα-苯基丙氨酰-[8-赖氨酸]加压素 > Nα-二甘氨酰-[8-赖氨酸]加压素 > Nα-脯氨酰-[8-赖氨酸]加压素 > Nα-三甘氨酰-[8-赖氨酸]加压素 > Nα-肌氨酰基甘氨酰-[8-赖氨酸]加压素。水解程度随着妊娠时间的延长逐渐增加，因为存在催产素。然而，加压素也在非孕妇血清中的酶的作用下被水解，但程度较小。在类似的分析条件下，催产素在非孕妇血清中不被水解，因此催产素比加压素更适合用于极谱测定血清催产素酶。

  DOI：

  10.1135/cccc19801099
• 作为产物：
  描述：

  (S)-1-[(S)-2-((S)-2-Amino-propionylamino)-propionyl]-pyrrolidine-2-carboxylic acid [(S)-1-(4-nitro-phenylcarbamoyl)-ethyl]-amide 在 musk melon protease 作用下， 以 水 为溶剂， 生成 L-丙氨酸4-硝基酰苯胺
  参考文献：
  名称：

  Kaneda, Makoto; Yonezawa, Hiroo; Uchikoba, Tetsuya, Bioscience, Biotechnology and Biochemistry, 1997, vol. 61, # 12, p. 2100 - 2102

  摘要：

  DOI：

文献信息

• Diamine derivatives as inhibitors of leukotriene A4 hydrolase
  申请人：Arnaiz Damian

  公开号：US20070155726A1

  公开（公告）日：2007-07-05

  This invention is directed to compounds of formula (I): where r, q, R, R 2 , R 3 , R 4 , R 5a , R 5b , R 5c , R 6a , R 6b , R 6c , R 7 , R 8 , and R 9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A 4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

  这项发明涉及式(I)的化合物： 其中r、q、R、R2、R3、R4、R5a、R5b、R5c、R6a、R6b、R6c、R7、R8和R9如本文所述，可以是单一立体异构体或立体异构体混合物，或其药学上可接受的盐、溶剂合物、包合物、多型体、铵离子、N-氧化物或其前药；这些化合物是白三烯A4水解酶抑制剂，因此在治疗炎症性疾病中有用。还公开了包括该发明化合物的药物组合物以及制备该发明化合物的方法。
• Specificity of a membrane-bound neutral endopeptidase from rat kidney.
  作者：YOSHIMITSU SHIMAMORI、YASUHIRO WATANABE、YUKIO FUJIMOTO

  DOI：10.1248/cpb.34.275

  日期：——

  The substrate specificity of a purified kidney neutral endopeptidase was studied. The endopeptidase hydrolyzed a variety of biologically active peptides, such as angiotensins (angiotensins I, II and III), bradykinins (bradykinin, Lys-bradykinin, Met-Lys-bradykinin and des-9Arg-bradykinin), enkephalins (Leu-enkephalin and Met-enkephalin), neurotensin and substance P, and was found to cleave only the bonds at the amino side of hydrophobic amino acids in the peptides. However, when a hydrophobic amino acid was present at the C-terminus or at the position adjacent to the N-terminus, the bond of the hydrophobic residue was not cleaved. In further studies on the degradation of a series of homo-oligopeptides, the enzyme appeared to hydrolyze those consisting of at least a tetrapeptide unit of hydrophobic amino acids such as Ala and Phe. The specificity of the membrane-bound neutral endopeptidase from rat kidney indicated by these results can be summarized as follows : the enzyme requires at least a tetrapeptide unit for hydrolysis, and cleavage occurs only at the amino side of a hydrophobic amino acid, when one is present at the third position of the tetrapeptide unit.

  纯化的肾脏中性内切肽酶的底物特异性被研究。该内切肽酶水解多种生物活性肽，如血管紧张素（血管紧张素I、II和III）、舒缓激肽（舒缓激肽、赖氨酸-舒缓激肽、甲硫氨酸-赖氨酸-舒缓激肽和去-9精氨酸-舒缓激肽）、脑啡肽（亮氨酸-脑啡肽和甲硫氨酸-脑啡肽）、神经降压素和P物质，并且发现它仅在肽中疏水氨基酸的氨基侧切割肽键。然而，当疏水氨基酸位于C末端或紧邻N末端的位置时，疏水残基的肽键不会被切割。在进一步研究一系列同源寡肽的降解过程中，该酶似乎水解那些至少由疏水氨基酸如丙氨酸和苯丙氨酸组成四肽单位的肽。根据这些结果，大鼠肾脏膜结合中性内切肽酶的特异性可以总结如下：酶需要至少一个四肽单位进行水解，并且仅在疏水氨基酸存在于四肽单位的第三位置时，才在该疏水氨基酸的氨基侧进行切割。
• [EN] NOVEL FAP INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE FAP
  申请人：UNIV ANTWERPEN

  公开号：WO2013107820A1

  公开（公告）日：2013-07-25

  The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.

  本发明涉及对FAP（成纤维细胞活化蛋白）具有高选择性和特异性的新型抑制剂。所述抑制剂可用作人类和/或兽药，特别是用于治疗和/或预防FAP相关疾病，如但不限于增殖性疾病。
• A 1010 Rate Enhancement of Phosphodiester Hydrolysis by a Dinuclear Aminopeptidase—Transition-State Analogues as Substrates?
  作者：Hyun Ik Park、Li-June Ming

  DOI：10.1002/(sici)1521-3773(19991004)38:19<2914::aid-anie2914>3.0.co;2-p

  日期：1999.10.4

  Streptomyces dizinc aminopeptidase (sAP) shows a specific activity of 33.7 nmol min(-1) mg(-1) toward the hydrolysis of the transition-state analogue bis-p-nitrophenylphosphate with a rate constant of k(cat)/K(m)=100 M(-1) s(-1) and a first-order rate enhancement of about 10(10), which is much superior to several Zn chemical models and comparable to some phosphodiesterases. This study suggests that

  链霉菌二锌氨基肽酶（sAP）对速率为k（cat）/ K（m）的过渡态类似物双-对硝基苯基磷酸酯的水解显示33.7 nmol min（-1）mg（-1）的比活性。 ）= 100 M（-1）s（-1）和约10（10）的一级速率增强，这比几种Zn化学模型要好得多，并且与某些磷酸二酯酶相当。这项研究表明，sAP可以作为一种新型的双核模型系统，以提供对双核水解的进一步了解。
• Purification of an Aminopeptidase Preferentially Releasing N-terminal Alanine from Cucumber Leaves and Its Identification as a Plant Aminopeptidase N
  作者：Yasuo YAMAUCHI、Yukinori EJIRI、Kiyoshi TANAKA

  DOI：10.1271/bbb.65.2802

  日期：2001.1

  In this study, a highly active foliar aminopeptidase preferentially releasing N-terminal alanine from artificial substrates was purified and characterized from cucumber (Cucumis sativus L. suyo). The enzyme had a molecular mass of 200 kDa consisting of two subunits of 95 kDa. It was a metalloprotease the pH optimum of which was 8 to 9. It cleaved Ala-, Gly-, Met-, Ser-, Leu-, Lys-, and Arg artificial substrates. An internal amino acid sequence was similar to those of aminopeptidase N (clan MA, family M1) of microorganisms, and was very similar to that of a putative aminopeptidase N of Arabidopsis thaliana. From these results, the highly active aminopeptidase in cucumber leaves was identified to be a plant aminopepitdase N.

  在本研究中，从黄瓜（Cucumis sativus L. suyo）中纯化和鉴定了一种高活性的叶面氨基肽酶，该酶优先从人工底物中释放N端丙氨酸。该酶的分子质量为200 kDa，由两个95 kDa的亚基组成。它是一种金属蛋白酶，其最适pH为8至9。它能切割Ala-、Gly-、Met-、Ser-、Leu-、Lys-和Arg的人工底物。其内部氨基酸序列与微生物的氨基肽酶N（MA家族，M1家族）相似，并且与拟南芥中假定的氨基肽酶N非常相似。根据这些结果，黄瓜叶中高活性的氨基肽酶被鉴定为植物氨基肽酶N。