(2R,4R,6R)-5-hydroxy-4-(hydroxymethyl)-3,7-dioxa-1,9-diazatricyclo[6.4.0.02,6]dodeca-8,11-dien-10-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: (2R,4R,6R)-5-hydroxy-4-(hydroxymethyl)-3,7-dioxa-1,9-diazatricyclo[6.4.0.02,6]dodeca-8,11-dien-10-one
• 化学式: C₉H₁₀N₂O₅
• 分子量: 226.19
• InChiKey: UUGITDASWNOAGG-RNMRRNDGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.5
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  91.6
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Novel Dideoxynucleoside Derivatives
  申请人：Kitade Yukio

  公开号：US20080064868A1

  公开（公告）日：2008-03-13

  The present invention discloses a 5′-amino-2′-fluoro-2′,5′-dideoxynucleoside derivative represented by the following formula [1]: (wherein R 1 represents a nucleic acid base which may have a protecting group; R 2 represents a hydrogen atom or a protecting group of an amino group; R 3 represents a hydrogen atom or a protecting group of a hydroxyl group); a dideoxynucleoside-insoluble carrier bound substance prepared by binding said dideoxynucleoside derivative to an insoluble carrier, and an oligonucleotide analogue into which said dideoxynucleoside derivative is introduced. The oligonucleotide analogue being introduced with a dideoxynucleoside derivative of the present invention has excellent thermal stability and also high binding affinity when duplex is formed. Also, it is anticipated that it has high resistance to nucleases. Further, the dideoxynucleoside derivative of the present invention can be used as an amidite reagent to be used for nucleic acid synthesis, and also as a starting material for solid phase synthesis of nucleic acid by binding the amidite reagent to a solid phase.

  本发明公开了由下式[1]所表示的5'-氨基-2'-氟-2',5'-二脱氧核苷衍生物（其中R1表示可能具有保护基团的核酸碱基；R2表示氢原子或氨基的保护基团；R3表示氢原子或羟基的保护基团）；通过将该二脱氧核苷衍生物与不溶性载体结合而制备的二脱氧核苷载体结合物质；以及引入了该二脱氧核苷衍生物的寡核苷酸类似物。本发明引入了含有该二脱氧核苷衍生物的寡核苷酸类似物具有优异的热稳定性，当形成双链时也具有高结合亲和力。此外，预计它具有高核酸酶抵抗力。此外，本发明的二脱氧核苷衍生物可用作用于核酸合成的酰胺酯试剂，也可作为将酰胺酯试剂结合到固相上进行核酸固相合成的起始物料。
• EMBODIMENTS OF A PROBE AND METHOD FOR TARGETING NUCLEIC ACIDS
  申请人：Hrdlicka Patrick Jerzy

  公开号：US20140220573A1

  公开（公告）日：2014-08-07

  Disclosed embodiments concern a probe comprising one or more pairs of monomers capable of targeting a nucleic acid target. The pair of monomers may be arranged in a manner that promotes thermoinstability of the probe complex, thus producing a probe capable of locating and/or detecting a target. The probe also may comprise one or more natural or non-natural nucleotides capable of Watson-Crick base pairing with an isosequential nucleic acid target. Particular disclosed embodiments concern a method of using the disclosed probe to target nucleic acids. In particular disclosed embodiments, the probe may be incubated with a target nucleic acid and then be detected.

  公开的实施例涉及一种探针，包括一个或多个能够定位到核酸靶标的单体对。这对单体可以被排列在一种促进探针复合物热不稳定性的方式下，从而产生一种能够定位和/或检测靶标的探针。该探针还可以包括一个或多个自然或非自然核苷酸，能够与同构核酸靶标进行Watson-Crick碱基配对。特定的实施例涉及使用所公开的探针来定位核酸的方法。在特定的实施例中，探针可以与靶向核酸一起孵育，然后被检测到。
• Nucleic Acid Labeling Compounds
  申请人：McGall Glenn

  公开号：US20110082289A1

  公开（公告）日：2011-04-07

  Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.
• Nucleic Acid Labelling Compounds
  申请人：McGall Glenn

  公开号：US20120053336A1

  公开（公告）日：2012-03-01

  Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.
• ANTISENSE OLIGONUCLEOTIDES WITH IMPROVED PHARMACOKINETIC PROPERTIES
  申请人：University of Vienna

  公开号：US20160193354A1

  公开（公告）日：2016-07-07

  The invention relates to an antisense or siRNA oligonucleotide or conjugate with improved pharmacokinetic properties, methods of producing the same as well as the use of such compounds and conjugates, e.g. as pharmaceutical composition, a pharmaceutical kit, a medicament or a tool in biomedical research. The conjugates of the invention have the formula I being P-(L-S-S-Y-X) n , wherein P represents a natural, artificial and/or modified oligonucleotide, L represents a linker group attached to one or more nucleosides at any position within the oligonucleotides sequence; S represents sulfur; X represents a ligand; Y represents a spacer and n is an integer ranging from 1 to the oligonucleotide length of P. The oligonucleotides of the invention have the formula II being P-(L-S-R) n , wherein P represents a natural, artificial and/or modified oligonucleotide, L represents a linker group attached to one or more nucleosides at any position within the oligonucleotides sequence, S represents sulfur, R represents either hydrogen or a thiol protecting group, preferably trityl or tertiary butyl, and n is an integer ranging from 1 to the oligonucleotide length of P. In addition, the pharmaceutical composition or pharmaceutical kit or conjugate can be used for the treatment of a disease or disorder that can be at least in part alleviated by therapy, wherein the disease or disorder is selected from the group consisting of bacterial infections, viral infections, cancer, metabolic diseases and immunological disorders and preferably cancer.