高等学校化学学报Issue(3)：531-537,7.DOI:10.7503/cjcu20130659
新型咪唑[2,1-b][1,3,4]噻二唑衍生物的合成及生物活性
Synthesis and Biological Activity of Novel Imidazo[2,1-b] [1,3,4] thiadiazole Derivatives
摘要
Abstract
To develop new β2-AR antagonists, eighteen novel 2,6-disubstituted imidazo[2,1-b] [1,3,4] thiadiazole derivatives containing 2-benzoxazolinone/benzothiazolinone moiety, 2-[ ( 2-benzoxazolinone/benzothiazolinone-3-yl)methyl]-6-aryl-imidazo[2,1-b] [1,3,4] thiadiazoles(5a-5i’), were synthesized by the condensation of compounds 4a and 4a’ with α-bromoarylketones under reflux in dry ethanol. Their structures of the newly synthesized compounds were confirmed by IR, 1 H NMR and elemental analysis. The target compounds were screened as β2-adrenergic receptor antagonist. The result indicated that some of them display obvious antagonistic effects toβ2-AR, and compound 5c’shows the highest antagonistic effect(70%). They can be considered as potential candidates as novel β2-AR antagonists.关键词
2-苯并噁/噻唑啉酮/咪唑2,1-b1,3,4噻二唑/β2-AR拮抗剂Key words
2-Benzoxazolinone/Benzothiazolinone/Imidazo [ 2 , 1-b ] [ 1 , 3 , 4 ] thiadiazole/β2-Adrenergic receptor antagonist分类
化学化工引用本文复制引用
李英俊,李春燕,靳焜,邵昕,周晓霞,李丽娜,赵楠,于洋,罗潼川..新型咪唑[2,1-b][1,3,4]噻二唑衍生物的合成及生物活性[J].高等学校化学学报,2014,(3):531-537,7.基金项目
辽宁省自然科学基金(批准号:20102126)资助.@@@@ Supported by the Natural Science Foundation of Liaoning Province, China(No.20102126) （批准号:20102126）
