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

作　　者：李英俊[1] 李春燕[1] 靳焜[2] 邵昕[1] 周晓霞[1] 李丽娜[1] 赵楠[1] 于洋[1] 罗潼川[1] 

机构地区：[1]辽宁师范大学化学化工学院,大连116029 [2]大连理工大学精细化工国家重点实验室,大连116012

出　　处：《高等学校化学学报》2014年第3期531-537,共7页Chemical Journal of Chinese Universities

基　　金：辽宁省自然科学基金(批准号:20102126)资助~~

摘　　要：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.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-b][1 3 4]噻二唑 β2-AR拮抗剂 

分 类 号：O626[理学—有机化学]