2-[(2-aminoethyl)thiomethyl]-3-hydroxy-pyridine | 52378-45-7

• 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: 2-[(2-aminoethyl)thiomethyl]-3-hydroxy-pyridine
• 英文别名: 3-hydroxy-2-((2-aminoethyl) thiomethyl)pyridine；2-((3-hydroxy-2-pyridyl)methylthio)ethylamine；2-{[(2-Aminoethyl)sulfanyl]methyl}pyridin-3-OL；2-(2-aminoethylsulfanylmethyl)pyridin-3-ol
• CAS: 52378-45-7
• 化学式: C₈H₁₂N₂OS
• 分子量: 184.262
• InChiKey: YTFSLUOQGOXGNB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  84.4
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-(4-methoxybenzyl)-2-methylthio-4-pyrimidone 、 2-[(2-aminoethyl)thiomethyl]-3-hydroxy-pyridine 生成 2-[2-[(3-hydroxypyridin-2-yl)methylsulfanyl]ethylamino]-5-[(4-methoxyphenyl)methyl]-1H-pyrimidin-6-one
  参考文献：
  名称：

  BROWN, T. H.;DURANT, G. J.;EMMETT, J. C.;GANELLIN, C. R.

  摘要：

  DOI：

文献信息

• Pyridyl alkylguanidine compounds, composition therewith, and methods of
  申请人：Smith Kline & French Laboratories Limited

  公开号：US03971786A1

  公开（公告）日：1976-07-27

  The compounds are pyridyl alkylguanidines, for example N-benzenesulphonyl-N'-methyl-N"-[2-((3-hydroxy-2-pyridyl)methylthio)ethyl] guanidine, which are inhibitors of histamine activity.

  这些化合物是吡啶基烷基胍，例如N-苯磺酰-N'-甲基-N"-[2-((3-羟基-2-吡啶基)甲硫基)乙基] 胍，它们是组织胺活性的抑制剂。
• Pharmaceutical compositions and methods of inhibiting H-1 and H-2
  申请人：Smith Kline & French Laboratories Limited

  公开号：US04000302A1

  公开（公告）日：1976-12-28

  Pharmaceutical compositions and methods of inhibiting H-1 and H-2 histamine receptors by administering an antihistamine and an H-2 histamine receptor inhibitor. Exemplary of the antihistamine in the compositions and methods of this invention is mepyramine and exemplary of the H-2 histamine receptor inhibitor is N-cyano-N'-methyl-N"-[2-((4-methyl-5-imidazolyl)-methylthio)ethyl]guanidin e.

  药物组合物和通过给予抗组胺药和H-2组胺受体抑制剂来抑制H-1和H-2组胺受体的方法。该发明的药物组合物和方法中的抗组胺药的示例是美匹拉明，H-2组胺受体抑制剂的示例是N-氰基-N'-甲基-N"-[2-((4-甲基-5-咪唑基)-甲硫基)乙基]胍。
• Ethylene derivatives
  申请人：Smith Kline & French Laboratories Limited

  公开号：US03953460A1

  公开（公告）日：1976-04-27

  The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-methylamino-2-[2-((4-methyl-5-imidazolyl) methylthio)ethylamino]-ethylene.

  这些化合物是乙烯衍生物，是组胺活性的抑制剂，特别是H-2组胺受体的抑制剂。本发明的一种化合物是1-硝基-2-甲基氨基-2-[2-((4-甲基-5-咪唑基)甲硫基)乙基氨基]-乙烯。
• 3-Nitro pyrrole compounds, processes for preparing them and pharmaceutical compositions containing them
  申请人：SMITH KLINE & FRENCH LABORATORIES LIMITED

  公开号：EP0005985A1

  公开（公告）日：1979-12-12

  This invention relates to nitro compounds which show activity as histamine H2-receptor antagonists. The compounds of the invention are of Structure where Het is an optionally substituted 5- or 6- membered fully-unsaturated heterocycle containing at least one nitrogen atom, or a furan or thiophene ring substituted by a substituted or unsubstituted aminoalkyl group; Z is sulfur, methylene or oxygen, m is 0, 1 or 2, n is 2 or 3 with m + n being 3 or 4; R3 is hydrogen or various substituents; and R" is hydrogen or lower alkyl; and acid addition salts thereof. The compounds can be prepared by condensing appropriate moieties containing the Het and pyrrole portions of the desired product. The compositions of the invention contain at least one of the compounds of the invention, and a pharmaceutical carrier.

  本发明涉及具有组胺 H2 受体拮抗剂活性的硝基化合物。本发明化合物的结构如下 其中 Het 是任选取代的含至少一个氮原子的 5-或 6-成员全不饱和杂环，或被取代或未取代的氨基烷基取代的呋喃或噻吩环；Z 是硫、亚甲基或氧，m 是 0、1 或 2，n 是 2 或 3，其中 m+n 是 3 或 4；R3 是氢或各种取代基；R "是氢或低级烷基；及其酸加成盐。这些化合物可以通过缩合含有所需产物的 Het 和吡咯部分的适当分子来制备。本发明的组合物含有至少一种本发明化合物和一种药物载体。
• Amidinosulphonic acid derivatives, process for their preparation and pharmaceutical compositions containing these derivatives
  申请人：SMITH KLINE & FRENCH LABORATORIES LIMITED

  公开号：EP0009061A1

  公开（公告）日：1980-04-02

  Amidino sulphonic acid compounds of the formula where Het is a nitrogen-containing 5 or 6 membered heterocyclic group, Z is sulphur or methylene, n is 2 or 3 and R is hydrogen, lower alkyl or Het CH2Z(CH2)n have activity as histamine H2-receptor antagonists and are the ingredients of pharmaceutical compositions. The compounds are prepared by primary amine coupling reactions. Compounds of the invention where Z is a methylene group can also be prepared by reacting the corresponding thiourea or sulphinic acid with an oxidising agent.

  式中的脒基磺酸化合物 其中 Het 是含氮的 5 或 6 位杂环基团，Z 是硫或亚甲基，n 是 2 或 3，R 是氢、低级烷基或 Het CH2Z(CH2)n 具有组胺 H2 受体拮抗剂的活性，是药物组合物的成分。这些化合物是通过伯胺偶联反应制备的。 Z 为亚甲基的本发明化合物也可通过相应的硫脲或亚硫酸与氧化剂反应制备。