新型含噁二唑环的苯并噁/噻唑啉酮衍生物的合成、表征及生物活性  

Synthesis and Biological Activities of Novel Benzoxazolinone/Benzothiazolone Derivatives Containing Oxadiazole Moiety

作　　者：李英俊[1] 李春燕[1] 靳焜[2] 孙淑琴[1] 周晓霞[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：《化学学报》2012年第2期151-160,共10页Acta Chimica Sinica

基　　金：辽宁省自然科学基金(No.20102126)资助项目~~

摘　　要：以邻氨基苯酚(硫酚)和尿素为起始原料,经一系列反应,合成出了30个新型含噁二唑环的苯并噁/噻唑啉酮衍生物(6).利用IR、1H NMR和元素分析对新化合物4和6的结构进行了表征.对所合成的目标化合物进行了抗癌、抗炎和免疫调节活性的筛选,实验结果表明,部分目标化合物具有弱的抗癌和免疫调节活性,对TNF-α和Cdc25B磷酸酯酶均无抑制活性.Thirty novel benzoxazolinone/benzothiazolone derivatives（6） containing oxadiazole moiety were synthesized by 2-aminophenol or 2-aminothiophenol and urea as starting materials via a series of reac-tions.The structures of new intermediate 4 and the target compounds 6 were characterized by IR,1H NMR spectra and elemental analysis.The synthesized target compounds were screened for the anticancer,antiin-flammatory and immunoregulatory activities.The results indicated that some compounds exhibited weak ac-tivities in the anticancer and immunoregulatory fields,while all of them were found to be inactive against TNF-α and Cdc25B phosphatase.

关 键 词：苯并噁/噻唑啉酮 噁二唑 合成 表征 生物活性 

分 类 号：O626.2[理学—有机化学]