2-acetylamino-5-(pyridin-2-ylthio)thiazole | 133691-58-4

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 英文名称: 2-acetylamino-5-(pyridin-2-ylthio)thiazole
• 英文别名: 2-acetylamino-5-(2-pyridylthio)thiazole；N-(5-pyridin-2-ylsulfanyl-1,3-thiazol-2-yl)acetamide
• CAS: 133691-58-4
• 化学式: C₁₀H₉N₃OS₂
• 分子量: 251.333
• InChiKey: FCHLVUGQEIZLAV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  108
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-acetylamino-5-(pyridin-2-ylthio)thiazole 在 盐酸 、 溶剂黄146 、 间氯过氧苯甲酸 作用下， 以 氯仿 为溶剂， 生成 2-amino-5-(pyridin-2-ylsulfinyl)thiazole
  参考文献：
  名称：

  Discovery of FR115092 : A novel antinephritic agent

  摘要：

  A series of dapsone-related 4-aminophenyl and 2-aminothiazolyl derivatives was prepared, and their antinephritic activity and blood toxicity were evaluated. 5-(2-Pyridylsulfonyl)-2-thiazolamine (FR115092, 26) was effective against two nephritis models, namely graft-versus-host disease (GVHD) and autoimmune W/BF1 mice, and showed none of the blood toxicity observed with dapsone. (C) 1997 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(97)10192-5
• 作为产物：
  描述：

  2-乙酰胺基噻唑 在 N-氯代丁二酰亚胺 、 potassium carbonate 、 溶剂黄146 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 2-acetylamino-5-(pyridin-2-ylthio)thiazole
  参考文献：
  名称：

  Discovery of FR115092 : A novel antinephritic agent

  摘要：

  A series of dapsone-related 4-aminophenyl and 2-aminothiazolyl derivatives was prepared, and their antinephritic activity and blood toxicity were evaluated. 5-(2-Pyridylsulfonyl)-2-thiazolamine (FR115092, 26) was effective against two nephritis models, namely graft-versus-host disease (GVHD) and autoimmune W/BF1 mice, and showed none of the blood toxicity observed with dapsone. (C) 1997 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(97)10192-5

文献信息

• Thiazole derivatives, processes for production thereof and
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US05256675A1

  公开（公告）日：1993-10-26

  Compounds of the formula: ##STR1## wherein A is S, SO, or SO2, R1 is H or acyl, R2 is H, alkyl, hydroxyalkyl, halogen or carboxy, and R3 is pyridyl are claimed. The compounds are useful as therapeutic agents for the treatment of e.g. rheumatism, nephritis and thrombocytopenia.

  该公式化合物为：##STR1## 其中A为S、SO或SO2，R1为H或酰基，R2为H、烷基、羟基烷基、卤素或羧基，R3为吡啶基。这些化合物可用作治疗药剂，用于治疗风湿病、肾炎和血小板减少症等疾病。
• Thiazole derivatives, processes for production thereof and pharmaceutical compositions comprising the same
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0412404A2

  公开（公告）日：1991-02-13

  A compound of the formula : wherein R¹ is hydrogen or acyl which may be substituted with halogen, R² is hydrogen, lower alkyl, hydroxy(lower)alkyl, halogen or carboxy, A is -CH₂-, -CO-, -C(=NOR⁴)- [wherein R⁴ is lower alkyl, [wherein m is 0, 1 or 2], and R³ is aryl which may be substituted with halogen, hydroxy, lower alkoxy, nitro, amino or acylamino; or N-containing unsaturated heterocyclic group which may be substituted with lower alkyl, amino, hydroxy or halo(lower)alkyl, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them as an active ingredient in admixture with pharmaceutically acceptable carriers.

  式中的化合物 其中 R¹ 是氢或可被卤素取代的酰基、 R² 是氢、低级烷基、羟基（低级）烷基、卤素或羧基、 A 是-CH₂-、-CO-、-C(=NOR⁴)-[其中 R⁴ 是低级烷基、 [其中 m 为 0、1 或 2]，以及 R³ 是可被卤素、羟基、低级烷氧基、硝基、氨基或酰氨基取代的芳基；或 可被低级烷基、氨基、羟基或卤代（低级）烷基取代的含 N 的不饱和杂环基团、 及其药学上可接受的盐类、 它们的制备工艺以及由它们作为活性成分与药学上可接受的载体混合而成的药物组合物。
• US5256675A
  申请人：——

  公开号：US5256675A

  公开（公告）日：1993-10-26
• US5369107A
  申请人：——

  公开号：US5369107A

  公开（公告）日：1994-11-29
• Discovery of FR115092 : A novel antinephritic agent
  作者：Takashi Ogino、Kiyoshi Tsuji、Takashi Tojo、Norihiro Igari、Nobuo Seki、Yu Sudo、Toshitaka Manda、Fusako Nishigaki、Masaaki Matsuo

  DOI：10.1016/s0960-894x(97)10192-5

  日期：1998.1

  A series of dapsone-related 4-aminophenyl and 2-aminothiazolyl derivatives was prepared, and their antinephritic activity and blood toxicity were evaluated. 5-(2-Pyridylsulfonyl)-2-thiazolamine (FR115092, 26) was effective against two nephritis models, namely graft-versus-host disease (GVHD) and autoimmune W/BF1 mice, and showed none of the blood toxicity observed with dapsone. (C) 1997 Elsevier Science Ltd. All rights reserved.