6-thiophen-2-yl-imidazo[2,1-b][1,3,4]thiadiazole-2-sulfonic acid amide | 63735-90-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 6-thiophen-2-yl-imidazo[2,1-b][1,3,4]thiadiazole-2-sulfonic acid amide
• 英文别名: 6-Thiophen-2-ylimidazo[2,1-b][1,3,4]thiadiazole-2-sulfonamide
• CAS: 63735-90-0
• 化学式: C₈H₆N₄O₂S₃
• 分子量: 286.359
• InChiKey: SKSLXMJJVLBPPJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  155
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-溴-1-(2-THIENYL)-1-ETHANONE 、 5-氨基-1,3,4-噻二唑-2-磺酰胺 以 乙醇 为溶剂， 反应 60.0h， 以35%的产率得到6-thiophen-2-yl-imidazo[2,1-b][1,3,4]thiadiazole-2-sulfonic acid amide
  参考文献：
  名称：

  Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 2. Imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamides

  摘要：

  A series of imidazo[2,1-b]thiadiazole and imidazo[2,1-b]thiazolesulfonamide carbonic anhydrase inhibitors is described and their anticonvulsant activities are listed. Many of the compounds have the same degree of ionization as acetazolamide and methazolamide, but their higher lipophilicity means that they are more able to penetrate into the central nervous system. One compound, 6-tert-butyl-2-sulfamoylimidazo[2,1-b]-1,3,4-thiadiazole (8, UK-15,454) had an anticonvulsant ED50 of 2.6 mg/kg when administered orally to mice. 8 selectively increased cerebral blood flow in animals without producing a high level of metabolic acidosis.

  DOI：

  10.1021/jm00176a003

文献信息

• Imidazo [2,1-b]-1,3,4-thiadiazole suflonamides
  申请人：Jaquith B. James

  公开号：US20050069492A1

  公开（公告）日：2005-03-31

  This invention relates to compounds of Formula (I) and the use of compounds of Formula (I) as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems.

  本发明涉及公式（I）的化合物以及在治疗中枢和周围神经系统的神经元疾病中使用公式（I）化合物作为神经保护剂的用途。
• Imidazo[2,1-b]-1,3,4-thiadiazole sulfonamides
  申请人：Jaquith B. James

  公开号：US20070088059A1

  公开（公告）日：2007-04-19

  This invention relates to compounds of Formula I and the use of compounds of Formula I as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems. Formula I:

  本发明涉及I式化合物及其在治疗中枢和周围神经系统神经元疾病中作为神经保护剂的应用。I式：
• IMIDAZO [2,1,-b]-1,3,4-THIADIAZOLE SULFONAMIDES
  申请人：JAQUITH James B.

  公开号：US20090042953A1

  公开（公告）日：2009-02-12

  This invention relates to compounds of Formula I and the use of compounds of Formula I as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous systems. Formula I:

  本发明涉及公式I化合物及其作为神经保护剂用于治疗中枢和外周神经系统的神经元疾病的用途。公式I：
• IMIDAZO[2,1-B]-1,3,4-THIADIAZOLE SULFONAMIDES
  申请人：Aegera Therapeutics Inc.

  公开号：EP1463735A1

  公开（公告）日：2004-10-06
• IMIDAZO¬2,1-B -1,3,4-THIADIAZOLE SULFONAMIDES
  申请人：Aegera Therapeutics Inc.

  公开号：EP1463735B1

  公开（公告）日：2009-08-12