1-(4,5-二甲基-1,3-噻唑-2-基)乙胺 | 432047-35-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 1-(4,5-二甲基-1,3-噻唑-2-基)乙胺
• 英文名称: 1-(4,5-dimethyl-1,3-thiazol-2-yl)-1-ethylamine
• 英文别名: 1-(4,5-dimethyl-1,3-thiazol-2-yl)ethanamine；1-(4,5-Dimethylthiazol-2-yl)ethanamine
• CAS: 432047-35-3
• 化学式: C₇H₁₂N₂S
• 分子量: 156.252
• InChiKey: VZQYBPGNBCABSI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  67.2
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2934100090

反应信息

• 作为反应物：
  描述：

  1-(4,5-二甲基-1,3-噻唑-2-基)乙胺 、 三光气 在 三乙胺 作用下， 以 氯仿 为溶剂， 反应 11.0h， 以100%的产率得到N-{4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2-methoxyphenyl}-N'-[1-(4,5-dimethyl-1,3-thiazol-2-yl)ethyl]urea
  参考文献：
  名称：

  EP1535910

  摘要：

  公开号：
• 作为产物：
  描述：

  在 溶剂黄146 、 锌 、 sodium hydroxide 作用下， 以 水 为溶剂， 生成 1-(4,5-二甲基-1,3-噻唑-2-基)乙胺
  参考文献：
  名称：

  New 1,2,4-triazine derivatives and biological applications thereof

  摘要：

  这项发明涉及公式(I)的新1,2,4-三嗪衍生物： 其中A、B、R2和Y在申请中有定义， 它们的制备和中间体，它们作为药物和药物组合物的用途以及含有它们的关联物。 公式(I)的化合物能够抑制细菌七糖合成。

  公开号：

  EP2141164A1

文献信息

• Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor
  申请人：Kubo Kazuo

  公开号：US20060235033A1

  公开（公告）日：2006-10-19

  An objective of the present invention is to provide compounds which have inhibitory activity against autophosphorylation of macrophage colony-stimulating factor receptors. The compounds of the present invention are represented by formula (I) and salt and solvate thereof: wherein X represents CH or N; Z represents O or S; R 1 , R 2 , and R 3 represent H, optionally substituted alkoxy or the like; R 4 represents H; R 5 , R 6 , R 7 , and R 8 represent H, halogen, alkyl, alkoxy, trifluoromethyl or the like; R 9 and R 10 represent H, alkyl or the like; and any one of R 11 and R 12 represents H with the other representing alkyl and R 13 represents an optionally substituted carbocyclic or heterocyclic ring or the like, or R 11 represents H and R 12 and R 13 combine together to form a bicyclic carbocyclic ring.

  本发明的目标是提供具有抑制巨噬细胞集落刺激因子受体自磷酸化活性的化合物。本发明的化合物由式（I）及其盐和溶剂化物表示：其中X表示CH或N；Z表示O或S；R1、R2和R3表示H、可选地取代的烷氧基或类似物；R4表示H；R5、R6、R7和R8表示H、卤素、烷基、烷氧基、三氟甲基或类似物；R9和R10表示H、烷基或类似物；R11和R12中的任意一个表示H，另一个表示烷基，R13表示可选地取代的碳环或杂环环或类似物，或R11表示H，R12和R13结合形成双环碳环。
• QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF MACROPHAGE COLONY STIMULATING FACTOR RECEPTOR
  申请人：KIRIN BEER KABUSHIKI KAISHA

  公开号：EP1535910A1

  公开（公告）日：2005-06-01

  An objective of the present invention is to provide compounds which have inhibitory activity against autophosphorylation of macrophage colony-stimulating factor receptors. The compounds of the present invention are represented by formula (I) and salt and solvate thereof: wherein X represents CH or N; Z represents O or S; R1, R2, and R3 represent H, optionally substituted alkoxy or the like; R4 represents H; R5, R6, R7, and R8 represent H, halogen, alkyl, alkoxy, trifluoromethyl or the like; R9 and R10 represent H, alkyl or the like; and any one of R11 and R12 represents H with the other representing alkyl and R13 represents an optionally substituted carbocyclic or heterocyclic ring or the like, or R11 represents H and R12 and R13 combine together to form a bicyclic carbocyclic ring.

  本发明的目的是提供对巨噬细胞集落刺激因子受体的自身磷酸化具有抑制活性的化合物。本发明的化合物由式（I）及其盐和溶液表示： 其中 X 代表 CH 或 N；Z 代表 O 或 S；R1、R2 和 R3 代表 H、任选取代的烷氧基或类似物；R4 代表 H；R5、R6、R7 和 R8 代表 H、卤素、烷基、烷氧基、三氟甲基或类似物；R9 和 R10 代表 H、烷基或类似物；R11 和 R12 中的任一个代表 H，另一个代表烷基，R13 代表任选取代的碳环或杂环或类似物，或 R11 代表 H，R12 和 R13 结合在一起形成双环碳环。
• Novel HldE-K Inhibitors Leading to Attenuated Gram Negative Bacterial Virulence
  作者：Nicolas Desroy、Alexis Denis、Chrystelle Oliveira、Dmytro Atamanyuk、Sophia Briet、Fabien Faivre、Géraldine LeFralliec、Yannick Bonvin、Mayalen Oxoby、Sonia Escaich、Stéphanie Floquet、Elodie Drocourt、Vanida Vongsouthi、Lionel Durant、François Moreau、Theodore B. Verhey、Ting-Wai Lee、Murray S. Junop、Vincent Gerusz

  DOI：10.1021/jm301499r

  日期：2013.2.28

  We report here the optimization of an HldE kinase inhibitor to low nanomolar potency, which resulted in the identification of the first reported compounds active on selected E. coli strains. One of the most interesting candidates, compound 86, was shown to inhibit specifically bacterial I,PS heptosylation on efflux pump deleted E. coli strains. This compound did not interfere with E. coli bacterial growth (MIC > 32 mu g/mL) but sensitized this pathogen to hydrophobic antibiotics like macrolides normally inactive on Gram-negative bacteria. In addition, 86 could sensitize E. coli to serum complement killing. These results demonstrate that HldE kinase is a suitable target for drug discovery. They also pave the way toward novel possibilities of treating or preventing bloodstream infections caused by pathogenic Gram negative bacteria by inhibiting specific virulence factors.
• US7598258B2
  申请人：——

  公开号：US7598258B2

  公开（公告）日：2009-10-06
• [EN] NEW 1,2,4-TRIAZINE DERIVATIVES AND BIOLOGICAL APPLICATIONS THEREOF<br/>[FR] NOUVEAUX DÉRIVÉS DE 1,2,4-TRIAZINE ET LEURS APPLICATIONS BIOLOGIQUES
  申请人：MUTABILIS SA

  公开号：WO2010001220A1

  公开（公告）日：2010-01-07

  The invention relates to new 1,2,4-triazine derivatives of formula (I): wherein A, B, R2 and Y are defined in the application, their preparation and intermediates, their use as drugs and pharmaceutical compositions and associations containing them. The compounds of formula (I) are capable of inhibiting bacterial heptose synthesis.