CAJ | 학술논문

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。
합성료18개신형함분병오/새서람동결구적2,6-이취대미서[2,1-b][1,3,4]새이서연생물5a~5i',즉2-[(2-분병오/새서람동-3-기)갑기]-6-방기-미서[2,1-b][1,3,4]새이서。이용홍외광보、핵자공진화원소분석대화합물적결구진행료표정。β2-신상선소수체(β2-AR)길항제개류사선결과표명,부분목표화합물대β2-AR구유명현적길항작용,기중화합물5c'적길항효과최고,위70%。저사화합물가작위잠재적β2-AR길항제。
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.