ethyl 5,6-diphenyl-3-[(4-sulamoyl)phenyl amino]pyridazine-4-carboxylate | 1403983-37-8

• 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: ethyl 5,6-diphenyl-3-[(4-sulamoyl)phenyl amino]pyridazine-4-carboxylate
• 英文别名: ethyl 5,6-diphenyl-3-(4-sulfamoylphenylamino)-4-pyridazinecarboxylate；Ethyl 5,6-diphenyl-3-(4-sulfamoylanilino)pyridazine-4-carboxylate
• CAS: 1403983-37-8
• 化学式: C₂₅H₂₂N₄O₄S
• 分子量: 474.54
• InChiKey: GDTNTANUAJUDDG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  34
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  133
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  异硫氰酸乙酯 、 ethyl 5,6-diphenyl-3-[(4-sulamoyl)phenyl amino]pyridazine-4-carboxylate 在 potassium hydroxide 作用下， 以 苯 为溶剂， 反应 6.0h， 以67%的产率得到ethyl 3-((4-(N-(ethylcarbamothioyl)sulfamoyl)phenyl)amino)-5,6-diphenylpyridazine-4-carboxylate
  参考文献：
  名称：

  Pyridazine and its related compounds. Part 34. Hypoglycemic and hypolipidemic activity of some novel condensed pyridazine sulfonamides

  摘要：

  A novel class of sulfonylurea and thiourea derivatives substituted with pyridazine and triazolopyridazine were designed and synthesized. The target compounds were assayed for their effects on the insulin release of alloxan-induced diabetic rats. The results showed that derivatives 4a, 4c, 8a, 11a, and 11b have significant antihyperglycemic effect in an experimental model of diabetes mellitus. No significant differences in cholesterol levels were observed between the diabetic group and diabetic groups that received the test compounds. However, the triglycerides level was reduced significantly by compound 8a when compared with the diabetic group.

  DOI：

  10.1007/s00044-013-0605-5
• 作为产物：
  描述：

  苯偶酰腙 以 正丁醇 为溶剂， 反应 3.0h， 生成 ethyl 5,6-diphenyl-3-[(4-sulamoyl)phenyl amino]pyridazine-4-carboxylate
  参考文献：
  名称：

  预期抗癌活性的噻吩并[2,3-c]哒嗪衍生物的设计与合成

  摘要：

  设计和合成一些新的噻吩并哒嗪衍生物作为抗癌剂是这项工作的目标。因此，通过使噻吩并哒嗪羧酸酰肼与不同的有机试剂反应，合成了一系列新型化合物。美国国家癌症研究所选择了十二种新化合物进行全面的抗癌筛选试验，其中七个被研究的化合物对所有癌细胞系均表现出非选择性的广谱和有希望的活性。选择了最具活性的化合物之一，以五个浓度水平针对60细胞株进行评估，并显示出显着的生长抑制活性。

  DOI：

  10.1007/s00044-012-0258-9

文献信息

• Design and synthesis of some thieno[2,3-c]pyridazine derivatives of expected anticancer activity
  作者：Afaf K. El-Ansary、Aliaa M. Kamal、Mokhtar AbdHafiz Al-Ghorafi

  DOI：10.1007/s00044-012-0258-9

  日期：2013.6

  Design and synthesis of some new thienopyridazine derivatives as anticancer agents were the goal of this work. Accordingly, a series of novel compounds were synthesized via reacting thienopyridazine carboxylic acid hydrazide with different organic reagents. Twelve novel compounds were selected by National Cancer Institute for a full anticancer screening assay where seven of the investigated compounds

  设计和合成一些新的噻吩并哒嗪衍生物作为抗癌剂是这项工作的目标。因此，通过使噻吩并哒嗪羧酸酰肼与不同的有机试剂反应，合成了一系列新型化合物。美国国家癌症研究所选择了十二种新化合物进行全面的抗癌筛选试验，其中七个被研究的化合物对所有癌细胞系均表现出非选择性的广谱和有希望的活性。选择了最具活性的化合物之一，以五个浓度水平针对60细胞株进行评估，并显示出显着的生长抑制活性。
• Pyridazine and its related compounds. Part 34. Hypoglycemic and hypolipidemic activity of some novel condensed pyridazine sulfonamides
  作者：Ali Deeb、Wafaa El-Eraky、Sally El-Awdan、Sebaey Mahgoub

  DOI：10.1007/s00044-013-0605-5

  日期：2014.1

  A novel class of sulfonylurea and thiourea derivatives substituted with pyridazine and triazolopyridazine were designed and synthesized. The target compounds were assayed for their effects on the insulin release of alloxan-induced diabetic rats. The results showed that derivatives 4a, 4c, 8a, 11a, and 11b have significant antihyperglycemic effect in an experimental model of diabetes mellitus. No significant differences in cholesterol levels were observed between the diabetic group and diabetic groups that received the test compounds. However, the triglycerides level was reduced significantly by compound 8a when compared with the diabetic group.