5-[(6-Methylimidazo[2,1-b][1,3]thiazol-5-yl)methylidene]-1,3-diazinane-2,4,6-trione

• 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: 5-[(6-Methylimidazo[2,1-b][1,3]thiazol-5-yl)methylidene]-1,3-diazinane-2,4,6-trione
• 化学式: C₁₁H₈N₄O₃S
• 分子量: 276.276
• InChiKey: WTYRVOAPMJHFPU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  121
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  巴比妥酸 、 6-甲基咪唑并[2,1-b]噻唑-5-甲醛 在 sodium acetate 、 溶剂黄146 作用下， 生成 5-[(6-Methylimidazo[2,1-b][1,3]thiazol-5-yl)methylidene]-1,3-diazinane-2,4,6-trione
  参考文献：
  名称：

  Synthesis and cardiotonic activity of imidazo[2,l-b]thiazoles bearing a lactam ring

  摘要：

  This paper describes the synthesis of 6-substituted imidazo[2,1-b] thiazoles with a lactam ring connected, by means of a methine group, to the 5-position. The pharmacological results show that interesting cardiotonic activity is obtained when the lactam ring is pseudothiohydantoin (8) or barbituric acid (9). Even the substituent at position 6 plays an important role in the pharmacological behavior of these derivatives. The following activity rank order was observed: phenyl > methyl > chlorine.

  DOI：

  10.1016/0223-5234(96)89164-1

文献信息

• BARBITURIC ACID ANALOGS AS THERAPEUTIC AGENTS
  申请人：DE BELIN Y. Jackie

  公开号：US20080113993A1

  公开（公告）日：2008-05-15

  This invention pertains to active barbituric acid analogs which inhibit HIF-1 activity (e.g., the interaction between HIF-1$g(a) and p300) and thereby inhibit angiogenesis, tumorigenesis, and proliferative conditions, such as cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HIF-1 activity, and to inhibit angiogenesis, tumorigenesis, and proliferative conditions, such as cancer.
• Synthesis and cardiotonic activity of imidazo[2,l-b]thiazoles bearing a lactam ring
  作者：A Andreani、M Rambaldi、A Leoni、A Locatelli、R Bossa、M Chiericozzi、I Galatulas、G Salvatore

  DOI：10.1016/0223-5234(96)89164-1

  日期：1996.1

  This paper describes the synthesis of 6-substituted imidazo[2,1-b] thiazoles with a lactam ring connected, by means of a methine group, to the 5-position. The pharmacological results show that interesting cardiotonic activity is obtained when the lactam ring is pseudothiohydantoin (8) or barbituric acid (9). Even the substituent at position 6 plays an important role in the pharmacological behavior of these derivatives. The following activity rank order was observed: phenyl > methyl > chlorine.