Synthesis, and Pharmacological Screening of Novel Sulfamoylphenylcarbamoylquinoxaline Derivatives as Anti-Inflammatory, Analgesic and Antitumour Agents
作者:Awatf Al-Said Farrag、Yousry Ahmed Ammar、Abd Allah Ghodran El-Sehemi、Hamdy Khamees Thabet、Nashwa Abd-Alim Hassan、Aziza Khalil Samy
DOI:10.3184/174751911x12983997221326
日期:2011.3
sulfonamides gave 3-sulfamoylphenylcarbamoylquinoxaline-2-carboxylic acid derivatives. While fusing the anhydride with the same sulfonamides produced the corresponding 3-sulfamoylphenylcarbamoylquinoxalines. On refluxing 3-sulfamoylphenylcarbamoyl derivatives with acetic anhydride gave the pyrrolo[3,4-d]quinoxaline derivatives. The imide linkage in the latter compound was opened via its reaction with
用一些磺酰胺处理喹喔啉-2,3-二羧酸酐得到3-氨磺酰基苯基氨基甲酰基喹喔啉-2-羧酸衍生物。同时将酸酐与相同的磺酰胺融合产生相应的 3-氨磺酰基苯基氨基甲酰基喹喔啉。3-氨磺酰基苯基氨基甲酰基衍生物与乙酸酐回流,得到吡咯并[3,4-d]喹喔啉衍生物。后一化合物中的酰亚胺键通过其在融合条件下与胺反应而打开,并获得喹喔啉-2,3-二酰胺。一些合成化合物的药理学评价表明,在慢性模型的抗炎活性中,3-[4-(N-嘧啶-2-基氨磺酰基)苯基]氨基甲酰基}喹喔啉-2-羧酸与参考物等效药物,消炎痛以及具有非致溃疡作用。与参考药物相比,所有测试的化合物都显示出中等的镇痛活性。受试化合物的抗肿瘤活性表明,3-[4-(N-(5-methylisoxazol-3-yl)sulfamoyl)phenyl]carbamoyl}quinoxaline-2-carb acid, 4-(1,3-dioxo-1H -pyrrolo[3