2-Amino-5-(dimethylamino)-5-oxopentanoic acid

• 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: 2-Amino-5-(dimethylamino)-5-oxopentanoic acid
• 化学式: C₇H₁₄N₂O₃
• 分子量: 174.2
• InChiKey: SMWQVIPJGSEJPA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.8
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  83.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1,8-萘二甲酸酐 、 2-Amino-5-(dimethylamino)-5-oxopentanoic acid 以 N,N-二甲基甲酰胺 为溶剂， 生成 5-(dimethylamino)-2-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)-5-oxopentanoic acid
  参考文献：
  名称：

  10.1039/d4gc01134a

  摘要：

  DOI：

  10.1039/d4gc01134a

文献信息

• AMINO ACID GROUP-MODIFIED ORGANOPOLYSILOXANE AND SILANE, AMINO ACID GROUP-CONTAINING COMPOUND, AND PRODUCTION METHOD THEREOF
  申请人：MORIYA Hiroyuki

  公开号：US20110144369A1

  公开（公告）日：2011-06-16

  An amino acid-modified organopolysiloxane is provided. It has an amino acid derivative bonded to at least one silicon atom of the organopolysiloxane segment constituting the backbone of the organopolysiloxane via an amide bond represented by the following general formula (1): wherein X and Y are independently a C 1-10 divalent hydrocarbon group; m is an integer of 0 to 4; R a is hydrogen atom, a monovalent hydrocarbon group containing 1 to 4 carbon atoms, or an organic group represented by the following general formula (2): (wherein R b is hydrogen atom, a C 1-7 monovalent hydrocarbon group, an alkaline metal, or an alkaline earth metal, and R c is independently hydrogen atom, hydroxy group, or a C 1-10 monovalent hydrocarbon group optionally containing oxygen atom, sulfur atom, or nitrogen atom); and Z is an organic group represented by the general formula (2).

  提供了一种氨基酸修饰的有机聚硅氧烷。它具有通过下列一般式(1)表示的酰胺键与构成有机聚硅氧烷主链的有机聚硅氧烷片段上的至少一个硅原子键合的氨基酸衍生物，其中X和Y分别是C1-10双价碳氢基团；m是0至4的整数；R是氢原子、含有1至4个碳原子的单价碳氢基团，或者由下列一般式(2)表示的有机基(其中R是氢原子、C1-7单价碳氢基团、碱金属或碱土金属，R独立地是氢原子、羟基，或者C1-10单价碳氢基团，可选地含有氧原子、硫原子或氮原子)；Z是由一般式(2)表示的有机基。
• TEMPLATE-FIXED PEPTIDOMIMETICS WITH CCR10 ANTAGONISTIC ACTIVITY
  申请人：Jung Francoise

  公开号：US20120283168A1

  公开（公告）日：2012-11-08

  Novel template-fixed β-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to antagonize the receptor CCR10. They can be used as medicaments to treat or prevent diseases or conditions in the area of dermatological and cutaneous disorders, inflammation, allergic disorders, respiratory diseases, diseases of the gastro-intestinal tract, ophthalmic diseases, haematology and cancer. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

  具有以下一般式(I)的小说模板固定β-发夹仿生肽，其中单个元素T或P是α-氨基酸残基，可以连接在任何方向上，具体取决于它们在链中的位置，如描述和索赔中所定义，及其盐，具有拮抗受体CCR10的特性。它们可用作药物，用于治疗或预防皮肤病和皮肤疾病、炎症、过敏性疾病、呼吸道疾病、胃肠道疾病、眼科疾病、血液学和癌症等领域。这些β-发夹仿生肽可以通过基于混合固相和溶液相合成策略的过程制备。
• Novel fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof
  申请人：Cytovia, Inc.

  公开号：US20020150885A1

  公开（公告）日：2002-10-17

  The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.

  本发明涉及新型荧光染料、新型荧光报告分子和新的酶测定方法，可以用于检测整个细胞、细胞系和来自任何生物体或器官的组织样本中参与凋亡的caspase和其他酶的活性。报告分子和测定方法可用于药物筛选程序，以识别在整个细胞或组织中作为caspase级联抑制剂或诱导剂的化合物。本文介绍的试剂和测定也可用于确定人类癌细胞对化疗药物治疗的化学敏感性。本发明还涉及新型荧光报告分子和新的酶测定方法，可用于检测第2型甲硫氨酸肽酶、二肽基肽酶IV、钙蛋白酶、氨肽酶、HIV蛋白酶、腺病毒蛋白酶、HSV-1蛋白酶、HCMV蛋白酶和HCV蛋白酶的活性。
• CYCLIC PEPTIDE COMPOUND HAVING HIGH MEMBRANE PERMEABILITY, AND LIBRARY CONTAINING SAME
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP3636807A1

  公开（公告）日：2020-04-15

  The present inventors have found that when screening for cyclic peptide compounds that can specifically bind to a target molecule, the use of a library including cyclic peptide compounds having a long side chain in the cyclic portion can improve the hit rate for cyclic peptide compounds that can specifically bind to the target molecule. Meanwhile, the present inventors have found that tryptophan and tyrosine residues, which have conventionally been used in oral low molecular-weight pharmaceuticals and are amino acid residues having an indole skeleton or a hydroxyphenyl group, are not suitable for peptides intended to attain high membrane permeability.

  本发明人发现，在筛选能与目标分子特异性结合的环肽化合物时，使用包括环状部分具有长侧链的环肽化合物库，可以提高能与目标分子特异性结合的环肽化合物的命中率。同时，本发明者发现色氨酸和酪氨酸残基不适合用于旨在获得高膜渗透性的肽，这两种残基通常用于口服低分子量药物，是具有吲哚骨架或羟基苯基的氨基酸残基。
• EP1026988A4
  申请人：——

  公开号：EP1026988A4

  公开（公告）日：2005-03-30

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