(R)-(+)-5-(1-methyl-2-pyrrolidinyl)-2(1H)-pyridone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: (R)-(+)-5-(1-methyl-2-pyrrolidinyl)-2(1H)-pyridone
• 英文别名: (R)-(+)-5-(1-methyl-2-pyrrolidinyl)-2-pyridone；5-[(2R)-1-methylpyrrolidin-2-yl]pyridin-2-ol
• 化学式: C₁₀H₁₄N₂O
• 分子量: 178.234
• InChiKey: ATRCOGLZUCICIV-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  32.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (R)-(+)-5-(1-methyl-2-pyrrolidinyl)-2(1H)-pyridone 在 Arthrobacter nicotinovorans 6-hydroxy-D-nicotine oxidase 作用下， 以 aq. buffer 为溶剂， 生成 6-羟基-N-甲基肌氨酸
  参考文献：
  名称：

  Turning a monocovalent flavoprotein into a bicovalent flavoprotein by structure-inspired mutagenesis

  摘要：

  A recently discovered class of bicovalent flavoproteins is an interesting group of enzymes because of their unusual cofactor binding mode, their open active sites and the bulky substrates they can accept. Through a sequence comparison study we have identified a conserved sequence region in bicovalent flavoproteins that is different from monocovalent flavoproteins. Based on this and the available structural information we have designed mutants of the prototype monocovalent flavoprotein, 6-hydroxy-D-nicotine oxidase (6HDNO), in order to introduce a second cofactor-protein linkage. Two amino acid replacements, namely histidine 130 to a cysteine and leucine 138 to a histidine, were sufficient to create a bicovalent 6HDNO. The introduced cysteine forms a covalent bond with FAD as found in natural bicovalent flavoproteins, while the second mutation was found to be essential to facilitate the formation of the cysteinyl linkage. This points to an important role of the introduced histidine in stabilizing a negative charge of the isoalloxazine ring during covalent flavinylation. The His130Cys/Leu138His 6HDNO is still active and shows a higher midpoint redox potential when compared to wild-type 6HDNO. This agrees well with the previous studies that have shown that bicovalent flavoenzymes have extremely high redox potentials (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2014.05.051

文献信息

• MATERIALS AND METHODS FOR IMMUNOASSAY OF PTERINS
  申请人：Adamczyk Maciej

  公开号：US20120115244A1

  公开（公告）日：2012-05-10

  Methods of assaying for (i) a pterin by immunoassay employing a pterin as capture agent, (ii) neopterin by chemiluminescent microparticle immunoassay (CMIA) employing an anti-neopterin antibody (Ab) as capture agent, (iii) neopterin by an immunoassay (IA) employing an acridinium (Acr)-labeled anti-neopterin Ab as conjugate, and (iv) neopterin by an IA employing Acr-labeled neopterin as tracer; an Acr-labeled anti-neopterin Ab; a conjugate/complex comprising anti-neopterin Ab and a carrier scaffold; a conjugated pterin; a conjugate comprising an Acr-labeled pterin and a carrier scaffold; an immunogen comprising neopterin and a carrier protein; a conjugate comprising such an immunogen and an Acr compound; an immunogen comprising a carrier protein and a neopterin hapten; a conjugate comprising such an immunogen and an Acr compound; a kit for assaying a pterin comprising a pterin as a capture agent and instructions for IA; and a kit for assaying neopterin comprising an anti-neopterin Ab as a capture agent and instructions for CMIA, neopterin comprising an Acr-labeled anti-neopterin Ab as a conjugate and instructions for IA, or Acr-labeled neopterin as a tracer and instructions for IA.

  测定(i)一种黄素的免疫测定方法，采用一种黄素作为捕获试剂，(ii)一种新生黄素的化学发光微粒免疫测定(CMIA)方法，采用一种抗新生黄素抗体(Ab)作为捕获试剂，(iii)一种新生黄素的免疫测定(IA)方法，采用一种荧光素(Acr)标记的抗新生黄素抗体作为结合物，以及(iv)一种新生黄素的免疫测定方法，采用Acr标记的新生黄素作为追踪物；一种Acr标记的抗新生黄素抗体；一种包含抗新生黄素抗体和载体支架的结合物/复合物；一种共轭的黄素；一种包含Acr标记的黄素和载体支架的结合物；一种含有新生黄素和载体蛋白的免疫原；一种包含这种免疫原和Acr化合物的结合物；一种含有载体蛋白和新生黄素半抗原的免疫原；一种包含这种免疫原和Acr化合物的结合物；一种黄素测定试剂盒，包括一种黄素作为捕获试剂和IA的说明书；以及一种新生黄素测定试剂盒，包括一种抗新生黄素抗体作为捕获试剂和CMIA的说明书，或者包括一种Acr标记的抗新生黄素抗体作为结合物和IA的说明书，或者包括一种Acr标记的新生黄素作为追踪物和IA的说明书。
• Stabilized highly unsaturated fatty acids and derivatives of such acids
  申请人：NABISCO BRANDS, INC.

  公开号：EP0338499A2

  公开（公告）日：1989-10-25

  Highly unsaturated fatty acid compounds, and derivatives thereof, are stabilized against oxidation with a water activated oxidoreductase enzyme. The fatty acid containing component is preferably microencapsulated in a wall member which comprises the enzyme.

  高度不饱和脂肪酸化合物及其衍生物在水活化氧化还原酶的作用下可防止氧化。含脂肪酸的成分最好微囊化在含有酶的壁件中。
• NOVEL NICOTINE DERIVATIVE
  申请人：JAPAN TOBACCO INC.

  公开号：EP0630904A1

  公开（公告）日：1994-12-28

  A novel nicotine derivative represented by general formula (1) wherein R represents a hexose or a dihexose; and (a) represents (S)-(-)-(3)-(1-methyl-2-pyrrolidinyl)-2-pyridyl, (R)-(+)-3-(1-methyl-2-pyrrolidinyl)-2-pyridyl, (S)-(-)-5-(1-methyl-2-pyrrolidinyl)-2-pyridyl, or (R)-(+)-5-(1-methyl-2-pyrrolidinyl)-2-pyridyl.

  由通式(1)代表的新型烟碱衍生物 其中 R 代表己糖或二己糖；代表(S)-(-)-(3)-(1-甲基-2-吡咯烷基)-2-吡啶基、(R)-(+)-3-(1-甲基-2-吡咯烷基)-2-吡啶基、(S)-(-)-5-(1-甲基-2-吡咯烷基)-2-吡啶基或(R)-(+)-5-(1-甲基-2-吡咯烷基)-2-吡啶基。
• NICOTINE DERIVATIVE
  申请人：JAPAN TOBACCO INC.

  公开号：EP0628567A1

  公开（公告）日：1994-12-14

  A novel sugar-containing nicotine derivative represented by general formula (1), wherein R represents a ribofuranosyl group; and X represents an oxygen atom or two hydrogen atoms. This compound is an excellent smoking taste modifier and has the effects of restoring the odor and taste of tobacco lost in the production of shredded tobacco and imparting a fine pattern of spreading to the smoke. Because the compound (1) has a characteristic structure containing ribofuranose in its molecule and also containing a physiologically active nicotine as the aglycon, it is expected to be used as a medicine with a reduced toxicity besides the smoking taste modifier. The invention also provides another novel nicotine derivative represented by general formula (2) wherein X is as defined above.

  一种新型含糖烟碱衍生物，由通式（1）表示，其中 R 代表一个核呋喃基团；X 代表一个氧原子或两个氢原子。这种化合物是一种极佳的烟味调节剂，具有恢复切丝烟草生产过程中损失的烟草气味和味道的作用，并能使烟雾呈现出细微的扩散模式。由于化合物(1)具有分子中含有核呋喃糖的特征结构，并且还含有具有生理活性的尼古丁作为苷元，因此除了作为烟味调节剂外，还有望用作毒性较低的药物。本发明还提供了由通式（2）表示的另一种新型尼古丁衍生物，其中 X 如上文所定义。
• Methods and kits for decreasing interferences from leukocytes in specific binding assays
  申请人：Yoshimura Toru

  公开号：US10641768B2

  公开（公告）日：2020-05-05

  The present disclosure describes methods and kits for reducing interferences in immunoassays performed on solid phase and on samples containing serum or plasma, by adding an effective amount of a polycationic derivative of dextran to the assay.

  本公开内容介绍了在固相和含有血清或血浆的样品上进行免疫测定时，通过在测定中添加有效量的右旋糖酐聚阳离子衍生物来减少干扰的方法和试剂盒。