Zhang Jin, Liu Jia, Ma Yangmin, Ren Decheng, Cheng Pei, Zhao Jiawen, Zhang Fan, Yao Yuan
College of Chemistry & Chemical Engineering, Shaanxi University of Science & Technology, Xi'an 710021, PR China; Key Laboratory of Auxiliary Chemistry & Technology for Chemical Industry, Ministry of Education, Xi'an 710021, PR China.
College of Chemistry & Chemical Engineering, Shaanxi University of Science & Technology, Xi'an 710021, PR China.
Bioorg Med Chem Lett. 2016 May 1;26(9):2273-7. doi: 10.1016/j.bmcl.2016.03.052. Epub 2016 Mar 25.
An efficient one-pot, three-component synthesis of quinazolinone derivatives containing 3-acrylamino motif was carried out using CeO2 nanoparticles as catalyst. Thirty-nine synthesized compounds were obtained with satisfied yield and elucidated by spectroscopic analysis. Four phytopathogenic fungi were chosen to test the antifungal activities by minimum inhibitory concentration (MIC) method. Compounds 4ag, 4bb, 4bc showed broad antifungal activities against at least three fungi, and dramatic effects of substituents on the activities were observed. Docking studies were established to explore the potential antifungal mechanism of quinazolinone derivatives as the chitinase inhibitors, and also verified the importance of the amide moiety.
以二氧化铈纳米颗粒为催化剂，高效地进行了一锅三组分合成含3-丙烯酰胺基序的喹唑啉酮衍生物的反应。得到了39个合成化合物，产率令人满意，并通过光谱分析进行了表征。选择了四种植物病原真菌，采用最低抑菌浓度（MIC）法测试其抗真菌活性。化合物4ag、4bb、4bc对至少三种真菌表现出广泛的抗真菌活性，并且观察到取代基对活性有显著影响。开展对接研究以探索喹唑啉酮衍生物作为几丁质酶抑制剂的潜在抗真菌机制，同时也验证了酰胺部分的重要性。
