(R,S)-O-benzyl-N-phenoxyacetylphenylalanine hydroxamate | 227020-20-4

• 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: (R,S)-O-benzyl-N-phenoxyacetylphenylalanine hydroxamate
• 英文别名: benzohydroxamic acid；2-[(2-phenoxyacetyl)amino]-3-phenyl-N-phenylmethoxypropanamide
• CAS: 227020-20-4
• 化学式: C₂₄H₂₄N₂O₄
• 分子量: 404.466
• InChiKey: NOZSDNJYPOIIJO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  30
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  76.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R,S)-O-benzyl-N-phenoxyacetylphenylalanine hydroxamate 在 palladium diacetate 氢气 作用下， 以 甲醇 为溶剂， 以56%的产率得到(R,S)-N-phenoxyacetylphenylalanine hydroxamate
  参考文献：
  名称：

  Hydroxamate Inhibitors ofAeromonas hydrophilaAE036 Metallo-B-lactamase

  摘要：

  Amino acid derived hydroxamates were synthesized and tested for inhibitory activity against different metallo-beta-lactamases. Several compounds inhibited the clinically relevant enzyme from Aeromonas hydrophila AE036. (C) 1999 Academic Press.

  DOI：

  10.1006/bioo.1998.1111
• 作为产物：
  描述：

  2-(2-苯氧基-乙酰氨基)-3-苯基-丙酸 在 三乙胺 、 N,N'-二环己基碳二亚胺 作用下， 以 二氯甲烷 、 乙酸乙酯 为溶剂， 生成 (R,S)-O-benzyl-N-phenoxyacetylphenylalanine hydroxamate
  参考文献：
  名称：

  Hydroxamate Inhibitors ofAeromonas hydrophilaAE036 Metallo-B-lactamase

  摘要：

  Amino acid derived hydroxamates were synthesized and tested for inhibitory activity against different metallo-beta-lactamases. Several compounds inhibited the clinically relevant enzyme from Aeromonas hydrophila AE036. (C) 1999 Academic Press.

  DOI：

  10.1006/bioo.1998.1111

文献信息

• ASSAYS, METHODS AND MEANS
  申请人：ISIS INNOVATION LIMITED

  公开号：US20150353646A1

  公开（公告）日：2015-12-10

  A novel class of hydroxylases is described having the amino acid sequence of SEQ ID NO: 2, 4, 6 and 8, and variants and fragments thereof having HIF hydroxylation activity. The polypeptides of the invention have in particular prolyl hydroxylase activity. An assay method monitors the interaction of the HIF hydroxylase with a substrate. Modulators of HIF hydroxylase are provided for use in the treatment of a condition associated with increased or decreased HIF levels or activity or for the treatment of a condition where it is desirable to modulate HIF levels or activity.

  描述了一类新型的羟化酶，具有序列编号为2、4、6和8的氨基酸序列，以及具有HIF羟化活性的变体和片段。该发明的多肽具有特别的脯氨酸羟化酶活性。一种测定方法监测HIF羟化酶与底物的相互作用。提供了HIF羟化酶的调节剂，用于治疗与HIF水平或活性增加或减少有关的疾病，或用于治疗需要调节HIF水平或活性的疾病。
• Assays, methods and means
  申请人：Maxwell Patrick Henry

  公开号：US20100272726A1

  公开（公告）日：2010-10-28

  A novel class of hydroxylases is described having the amino acid sequence of SEQ ID NO: 2, 4, 6 and 8, and variants and fragments thereof having HIF hydroxylation activity. The polypeptides of the invention have in particular prolyl hydroxylase activity. An assay method monitors the interaction of the HIF hydroxylase with a substrate. Modulators of HIF hydroxylase are provided for use in the treatment of a condition associated with increased or decreased HIF levels or activity or for the treatment of a condition where it is desirable to modulate HIF levels or activity.

  本文描述了一种新型的羟化酶，其氨基酸序列为SEQ ID NO：2、4、6和8，以及具有HIF羟化活性的变体和片段。本发明的多肽特别具有脯氨酸羟化酶活性。一种测定方法监测HIF羟化酶与底物的相互作用。提供了HIF羟化酶的调节剂，用于治疗与HIF水平或活性增加或减少相关的疾病，或用于治疗需要调节HIF水平或活性的疾病。
• Assays, Methods and Means
  申请人：Isis Innovation Limited

  公开号：US20140294842A1

  公开（公告）日：2014-10-02

  A novel class of hydroxylases is described having the amino acid sequence of SEQ ID No. 2, 4, 6 and 8, and variants and fragments thereof having HIF hydroxylation activity. The polypeptides of the invention have in particular prolyl hydroxylase activity. An assay method monitors the interaction of the HIF hydroxylase with a substrate. Modulators of HIF hydroxylase are provided for use in the treatment of a condition associated with increased or decreased HIF levels or activity or for the treatment of a condition where it is desirable to modulate HIF levels or activity.

  本文介绍了一类新型羟化酶，其氨基酸序列为SEQ ID No. 2、4、6和8及其变异体和片段，具有HIF羟化活性。本发明的多肽特别具有脯氨酸羟化酶活性。一种检测方法监测HIF羟化酶与底物的相互作用。提供用于治疗与HIF水平或活性增加或减少有关的疾病或治疗需要调节HIF水平或活性的疾病的HIF羟化酶调节剂。
• ASSAYS, METHODS AND MEANS RELATING TO HYPOXIA INDUCIBLE FACTOR (HIF) HYDROXYLASE
  申请人：ISIS INNOVATION LIMITED

  公开号：EP1379630B1

  公开（公告）日：2012-09-26
• US8535899B2
  申请人：——

  公开号：US8535899B2

  公开（公告）日：2013-09-17