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

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.

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

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.