N-芳基-4-(吡啶-2-基)-5-(1H-1,2,4-三唑-1-基)噻唑-2-胺衍生物的合成及生物活性研究

Synthesis and Biological Evaluation of N-Phenyl-4-(pyridin-2-yl)-5-(1H-1,2,4-triazol-1-yl)thiazol-2-amines

利用Hantzsch反应合成了13个N-芳基-4-(吡啶-2-基)-5-(1H-1,2,4-三唑-1-基)噻唑-2-胺衍生物,所有化合物的结构均经1H NMR,MS及元素分析确证.研究发现,溶剂对不同取代基的目标化合物的合成影响很大.生物活性测试结果表明,化合物均具有一定的杀菌活性.其中,化合物6c对番茄早疫和苹果轮纹、化合物6g对番茄早疫、化合物6h对黄瓜黑腥及化合物6i对苹果轮纹均显示80%以上的杀菌活性.

Thirteen new N-phenyl-4-（pyridin-2-yl）-5-（1H-1, 2, 4-triazol-1-yl）thiazol-2-amines were synthesized using Hantzsch reaction. Their structures of all these new compounds have been confirmed with 1H NMR spectra, MS and elemental analysis. It is found that the solvent used in the reaction has impotent influence on the synthesis of the title compounds containing different substituent. Their results of bioassay showed that all title compounds exhibited some degree of antifungal activities. Compound 6c against A. solani and P. piricola, compound 6g against A. solani, compound 6h against C. cucumerinum compound 6i against P. piricola displayed above 80% inhibition, respectively.