新型N-芳基亚甲基-N-(4-取代苯甲酰氧基噻唑-2-基)取代苯甲酰腙的合成与生物活性有机化学.pdfVIP

DOI: 10.6023/cjoc201408036 研究简报 有机化学 Chinese Journal of Organic Chemistry NOTE 新型N-芳基亚甲基-N-(4-取代苯甲酰氧基噻唑-2-基)取代苯甲酰腙的 合成与生物活性 刘建超 刘勇军 贺红武* (华中师范大学化学学院 武汉 430079) 摘要 利用生物活性亚结构拼接原理, 将活性酰腙亚结构与活性噻唑环亚结构进行拼接, 设计合成了 14 个新型 N-芳 基亚甲基-N-(4-取代苯甲酰氧基噻唑-2-基)取代苯甲酰腙衍生物. 所有目标化合物经 1H NMR 、IR 、质谱及元素分析等 手段进行了表征, 部分化合物还经过 13C NMR 进行了确证. 抗肿瘤测试结果表明, 该系列化合物表现出明显的抗肿瘤 活性, 其对人口腔上皮癌细胞株(KB) 的抑制活性优于对鼻咽癌细胞株(CNE2) 的抑制活性; 采用离体平皿法对目标化合 物进行杀菌活性测试, 测试菌种为: 小麦赤霉菌、水稻纹枯霉菌、黄瓜灰霉菌、番茄早疫菌、烟草赤星菌和黄瓜炭疽 菌. 结果表明, 在 1.0×10－4 g/mL 浓度下, 目标化合物对部分菌种表现中等抑菌活性. 关键词 噻唑; 酰腙; 抗肿瘤活性; 杀菌活性 Synthesis and Biological Evaluation of Novel N-Arylmethylene- N-(4-benzoyloxy-thiazole-2-yl) Benzoylhydrazone Derivatives Liu, Jianchao Liu, Yongjun He, Hongwu* (College of Chemistry, Central China Normal University, Wuhan 430079) Abstract 14 novel N-arylmethylene-N-(4-benzoyloxy-thiazole-2-yl) benzoylhydrazone derivatives were designed and syn- thesized by incorporating the activated structural templets of thiazole and acylhydrazone. All the target compounds were char- acterized by 1H NMR, IR, mass spectrometry and elemental analysis, and some of the compounds were confirmed by 13C NMR. Anti-tumor test results showed that the hydrazone compounds showed significant anti-tumor activity. These compounds were more active against the KB cell lines than the CNE2 cell lines. All synthesized compounds were screened by plate meth- od in vitro for