Key Laboratory of Pesticide & Chemical Biology, College of Chemistry, Ministry of Education, Central China Normal University, Wuhan 430079, PR China.
Bioorg Med Chem Lett. 2012 Feb 1;22(3):1455-8. doi: 10.1016/j.bmcl.2011.11.115. Epub 2011 Dec 4.
A novel synthetic method of N-cyanocarboxamides has been developed with advantages of mild reaction condition, simpler procedure and easy reactant-product isolation compared with the existing methods. Using this novel method, 16 new N-cyano-1H-imidazole-4-carboxamide derivatives were synthesized and their structures were characterized by spectrum analysis. Further antifungal activity study showed that most of the newly synthesized compounds have good antifungal activity selectively against Rhizoctonia solani among the six fungi tested. Particularly, compound 12h was identified as the most promising candidate with an EC(50) of 2.63 μg/mL against R. solani.
一种新型的 N-氰基甲酰胺的合成方法已经被开发出来,与现有的方法相比,该方法具有反应条件温和、步骤更简单、反应物-产物易于分离等优点。利用这种新方法,合成了 16 种新型的 N-氰基-1H-咪唑-4-甲酰胺衍生物,并通过光谱分析对其结构进行了表征。进一步的抗真菌活性研究表明,在所测试的六种真菌中,大多数新合成的化合物对茄病镰刀菌具有良好的选择性抗真菌活性。特别是化合物 12h 被鉴定为最有前途的候选物,其对茄病镰刀菌的 EC(50)为 2.63μg/mL。