1-{4-[(2-氰基亚胺基-1,3-噻唑烷-3-基)甲基]-噻唑-2-基}-3-取代苯甲酰基脲类化合物的合成及其生物活性  

Synthesis and Biological Activity of 1-{4-[(2-Cyanoimino-1,3-thiazolidine-3-yl)methyl]thiazol-2-yl}-3-aroyl Ureas

作　　者：戴红[1] 赵元飞[1] 牛平[1] 钱翊钧[1] 李永强[2] 方建新[2] 石玉军[1] 

机构地区：[1]南通大学化学化工学院,南通226019 [2]南开大学元素有机化学研究所,天津300071

出　　处：《有机化学》2013年第7期1568-1572,共5页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.21102077;21202089);国家级大学生创新训练计划项目(No.201210304039);江苏省"六大人才高峰"(No.2011-SWYY-009)资助项目~~

摘　　要：为了从噻唑类化合物中寻找新的活性物质,利用4-[(2-氰基亚胺基-1,3-噻唑烷-3-基)甲基]-2-氨基噻唑与芳酰基异氰酸酯的缩合反应,合成了一系列未见文献报道的新型含酰基脲结构的噻唑类衍生物6.经1H NMR,MS和元素分析对所有目标化合物的结构进行了表征,此外,经13C NMR进一步证实了化合物6a,6e及6h的结构.初步生物活性试验结果表明,在浓度为50μg/mL时,部分目标化合物表现出一定的杀菌活性.如化合物6d对小麦赤霉的抑制率为65.3%;化合物6f对花生褐斑的抑制率为67.3%;化合物6g对苹果轮纹的抑制率为56.1%.In search of novel thiazole derivatives with potent biological activities, a series of new thiazole compounds 6 con- taining acyl urea moiety were synthesized by the condensation of 2-cyanoimino-3-（2-aminothiazol-4-ylmethyl）thiazolidine with various arylacylisocyanates. The structures of the target compounds were determined by 1H NMR, MS and elemental analysis. The structures of 6a, 6e and 6h were further characterized by 13C NMR spectra. The bioassay data indicated that some of the title compounds showed fungicidal activities to some extent at the concentration of 50 ~tg/mL. For example, com- pound 6d displayed 65.3% inhibition rate against Gibberella zeae, compound 6f exhibited 67.3% inhibition rate against Cer- cospora arachidicola, and comt3ound 62 showed 56.1% inhibition rate against PkvsaloxtTora nirieola

关 键 词：酰基脲 噻唑 合成 生物活性 

分 类 号：O626[理学—有机化学]