论文部分内容阅读
合成了18个新型含苯并噁/噻唑啉酮结构的2,6-二取代咪唑[2,1-b][1,3,4]噻二唑衍生物5a~5i’,即2-[(2-苯并噁/噻唑啉酮-3-基)甲基]-6-芳基-咪唑[2,1-b][1,3,4]噻二唑.利用红外光谱、核磁共振和元素分析对化合物的结构进行了表征.β2-肾上腺素受体(β2-AR)拮抗剂钙流筛选结果表明,部分目标化合物对β2-AR具有明显的拮抗作用,其中化合物5c’的拮抗效果最高,为70%.这些化合物可作为潜在的β2-AR拮抗剂.
Eighteen novel 2,6-disubstituted imidazo [2,1-b] [1,3,4] thiadiazole derivatives 5a ~ 5i ’were synthesized with 18 new benzoxadiazole / (2-benzoxazepin-3-yl) methyl] -6-aryl-imidazo [2,1-b] [1,3,4] thiadiazole. Elemental analysis showed that the structure of the compound was characterized.The results of calcium screening of β2-adrenergic receptor (β2-AR) antagonist showed that some of the compounds showed obvious antagonistic effect on β2-AR, of which compound 5c showed the highest antagonistic effect , 70%. These compounds are potential β2-AR antagonists.