4-取代苯甲酰氧基-2-取代苯甲酰氨基噻唑衍生物的合成与生物活性  

Synthesis and biological evaluation of 4-benzoyloxy-2-benzoylamino-thiazole derivatives

作　　者：刘勇军[1] 张莎莎[1] 刘建超[1] 贺红武[1] 

机构地区：[1]华中师范大学化学学院,武汉430079

出　　处：《华中师范大学学报（自然科学版）》2015年第5期730-734,共5页Journal of Central China Normal University：Natural Sciences

基　　金：国家重点基础研究发展规划项目(2010CB126100);国家自然科学基金项目(21172090;31000867);教育部创新团队项目(IRT0953)

摘　　要：以商品化的杀菌剂噻唑菌胺和噻氟酰胺为先导,保持噻唑环活性结构,在噻唑环的4位引入酯基,设计合成了9个新型的4-取代苯甲酰氧基-2-取代苯甲酰氨基噻唑衍生物,中间体2-亚氨基-4-噻唑烷酮由简便易得的原料溴乙酸乙酯与硫脲一步合成.用IR、1 H NMR、13 C NMR、MS和元素分析等对合成的噻唑酰胺化合物结构进行了表征.并对其杀菌和抗肿瘤生物活性进行了测试,初步的研究结果表明,该类化合物基本上没有抗肿瘤活性,但部分化合物对小麦赤霉病和黄瓜灰霉病有较好的抑制效果.In this paper, a series of thiazole derivatives containing the activated structural templets of ethaboxam and trifluzamide were designed and synthesized. All the target compounds were characterized by methods such as 1H NMR, IR, elemental analysis, ^13C NMR and mass spectrometry. The intermediate 2-imino-4-oxo-thiazolinone was synthesized in one step using thiourea and ethyl 2-b were subjected to the screening test against sults showed that some compounds had good Gibberella zeae , Botrytis cinereapers. romoacetate. Most of the target compounds tumors and funguses, and the bioassay re biological activity such as fungicide against

关 键 词：噻氟酰胺 噻唑菌胺 苯甲酰氧基 噻唑化合物 杀菌 抗肿瘤 

分 类 号：O626.2[理学—有机化学]