5-nitro-cytidine | 120883-87-6

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷
• 英文名称: 5-nitro-cytidine
• 英文别名: 5-Nitro-cytidin；5-Nitrocytidin；5-Nitrocytidine；4-amino-1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-nitropyrimidin-2-one
• CAS: 120883-87-6
• 化学式: C₉H₁₂N₄O₇
• 分子量: 288.217
• InChiKey: NGCMLYZVLNLYTA-UAKXSSHOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  174
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  5-nitro-cytidine 在 磷酸三甲酯 、 Proton Sponge 、 三氯氧磷 、 三正丁胺 、 三丁基焦磷酸铵 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 2.03h， 生成 5-nitrocytidine-5'-triphosphate
  参考文献：
  名称：

  Synthesis and Antiviral Activity of 5-Substituted Cytidine Analogues:  Identification of a Potent Inhibitor of Viral RNA-Dependent RNA Polymerases

  摘要：

  As part of our studies of lethal viral mutagens, a series of 5-substituted cytidine analogues were synthesized and evaluated for antiviral activity. Among the compounds examined, 5-nitrocytidine was effective against poliovirus (PV) and coxsackievirus B3 (CVB3) and exhibited greater activity than the clinically employed drug ribavirin. Instead of promoting viral mutagenesis, 5-nitrocytidine triphosphate inhibited PV RNA-dependent RNA polymerase (K-d = 1.1 +/- 0.1 mu M), and this inhibition is sufficient to explain the observed antiviral activity.

  DOI：

  10.1021/jm060872x
• 作为产物：
  描述：

  2-(4-amino-5-nitro-2-oxopyrimidin-1(2H)-yl)-5((benzoyloxy)methyl)tetrahydrofuran-3,4-diyl dibenzoate 在 sodium hydroxide 作用下， 以 乙醇 为溶剂， 反应 3.0h， 以52%的产率得到5-nitro-cytidine
  参考文献：
  名称：

  Synthesis and Antiviral Activity of 5-Substituted Cytidine Analogues:  Identification of a Potent Inhibitor of Viral RNA-Dependent RNA Polymerases

  摘要：

  As part of our studies of lethal viral mutagens, a series of 5-substituted cytidine analogues were synthesized and evaluated for antiviral activity. Among the compounds examined, 5-nitrocytidine was effective against poliovirus (PV) and coxsackievirus B3 (CVB3) and exhibited greater activity than the clinically employed drug ribavirin. Instead of promoting viral mutagenesis, 5-nitrocytidine triphosphate inhibited PV RNA-dependent RNA polymerase (K-d = 1.1 +/- 0.1 mu M), and this inhibition is sufficient to explain the observed antiviral activity.

  DOI：

  10.1021/jm060872x

文献信息

• [EN] SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF<br/>[FR] NUCLÉOSIDES, NUCLÉOTIDES SUBSTITUÉS ET LEURS ANALOGUES
  申请人：ALIOS BIOPHARMA INC

  公开号：WO2014209979A1

  公开（公告）日：2014-12-31

  Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a norovirus, with a nucleoside, a nucleotide and an analog thereof.

  本文揭示了核苷、核苷酸及其类似物，包括一个或多个核苷、核苷酸及其类似物的药物组合物，以及它们的合成方法。本文还揭示了利用核苷、核苷酸及其类似物改善和/或治疗疾病和/或病况的方法，包括使用核苷、核苷酸和其类似物治疗诺如病毒感染的方法。
• [EN] CATIONIC LIPIDS AND USES THEREOF<br/>[FR] LIPIDES CATIONIQUES ET LEURS UTILISATIONS
  申请人：FACTOR BIOSCIENCE INC

  公开号：WO2021003462A1

  公开（公告）日：2021-01-07

  The present invention relates to novel cationic lipids of formula I, and more specifically formula IV. These are used, for example, in liposomes for the delivery of nucleic acids to cells.

  本发明涉及新型公式I的阳离子脂质，更具体地是公式IV。例如，这些脂质可用于脂质体中将核酸传递给细胞。
• SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF
  申请人：Alios BioPharma, Inc.

  公开号：US20150011497A1

  公开（公告）日：2015-01-08

  Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a norovirus, with a nucleoside, a nucleotide and an analog thereof.

  本文披露了核苷、核苷酸及其类似物、包括一个或多个核苷、核苷酸及其类似物的药物组合物以及其合成方法。本文还披露了使用核苷、核苷酸和其类似物来改善和/或治疗疾病和/或病况，包括由诺如病毒引起的感染的方法。
• METHODS AND PRODUCTS FOR TRANSFECTING CELLS
  申请人：FACTOR BIOSCIENCE INC.

  公开号：US20140356906A1

  公开（公告）日：2014-12-04

  The present invention relates in part to nucleic acids encoding proteins, nucleic acids containing non-canonical nucleotides, therapeutics comprising nucleic acids, methods, kits, and devices for inducing cells to express proteins, methods, kits, and devices for transfecting, gene editing, and reprogramming cells, and cells, organisms, and therapeutics produced using these methods, kits, and devices. Methods for inducing cells to express proteins and for reprogramming and gene-editing cells using RNA are disclosed. Methods for producing cells from patient samples, cells produced using these methods, and therapeutics comprising cells produced using these methods are also disclosed.

  本发明部分涉及编码蛋白质的核酸、含非规范核苷酸的核酸、包含核酸的治疗剂、诱导细胞表达蛋白质的方法、试剂盒和装置、转染、基因编辑和重编程细胞的方法、试剂盒和装置，以及使用这些方法、试剂盒和装置生产的细胞、生物体和治疗剂。公开了使用RNA诱导细胞表达蛋白质、重编程和基因编辑细胞的方法。还公开了从患者样本中制备细胞的方法、使用这些方法制备的细胞以及包含使用这些方法制备的细胞的治疗剂。
• Methods and products for nucleic acid production and delivery
  申请人：Factor Bioscience Inc.

  公开号：US10124042B2

  公开（公告）日：2018-11-13

  The present invention relates in part to nucleic acids, including nucleic acids encoding proteins, therapeutics and cosmetics comprising nucleic acids, methods for delivering nucleic acids to cells, tissues, organs, and patients, methods for inducing cells to express proteins using nucleic acids, methods, kits and devices for transfecting, gene editing, and reprogramming cells, and cells, organisms, therapeutics, and cosmetics produced using these methods, kits, and devices. Methods and products for altering the DNA sequence of a cell are described, as are methods and products for inducing cells to express proteins using synthetic RNA molecules, including cells present in vivo. Therapeutics comprising nucleic acids encoding gene-editing proteins are also described.

  本发明部分涉及核酸，包括编码蛋白质的核酸，包含核酸的治疗剂和化妆品，向细胞、组织、器官和患者提供核酸的方法，使用核酸诱导细胞表达蛋白质的方法，用于转染、基因编辑和重编程细胞的方法、试剂盒和装置，以及使用这些方法、试剂盒和装置生产的细胞、生物体、治疗剂和化妆品。本文描述了改变细胞 DNA 序列的方法和产品，以及使用合成 RNA 分子诱导细胞（包括体内细胞）表达蛋白质的方法和产品。此外，还介绍了包含编码基因编辑蛋白的核酸的治疗方法。