Gao Xingwen, Cai Xuejian, Yan Kai, Song Baoan, Gao Lili, Chen Zhuo
Center for Research and Development of Fine Chemicals, Guizhou University, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guiyang, 550025, PR China.
Molecules. 2007 Dec 27;12(12):2621-42. doi: 10.3390/12122621.
A simple and general method has been developed for the synthesis of various4(3H)-quinazolinone derivatives by the treatment of the appropriate 3-amino-2-aryl-4(3H)-quinazolinone with a substituted benzaldehyde in ethanol. The structures of the compoundswere characterized by elemental analysis, IR, (1)H-NMR and (13)C-NMR spectra. The title 2-aryl- or 2-methyl-3-(substituted-benzalamino)-4(3H)-quinazolinone compounds III-1~III-31 were found to possess moderate to good antiviral activity. Semi-quantitative PCR andReal Time PCR assays were used to ascertain the target of action of compound III-31against TMV. The studies suggest that III-31 possesses antiviral activity due to inductionof up-regulation of PR-1a and PR-5, thereby inhibiting virus proliferation and movementby enhancement of the activity of some defensive enzyme.
已开发出一种简单通用的方法，通过在乙醇中用取代的苯甲醛处理适当的3-氨基-2-芳基-4(3H)-喹唑啉酮来合成各种4(3H)-喹唑啉酮衍生物。通过元素分析、红外光谱、(1)H-NMR和(13)C-NMR光谱对化合物的结构进行了表征。发现标题化合物2-芳基或2-甲基-3-(取代苯亚甲基氨基)-4(3H)-喹唑啉酮化合物III-1~III-31具有中等至良好的抗病毒活性。使用半定量PCR和实时PCR测定法来确定化合物III-31对烟草花叶病毒（TMV）的作用靶点。研究表明，III-31具有抗病毒活性是由于诱导了PR-1a和PR-5的上调，从而通过增强一些防御酶的活性来抑制病毒增殖和移动。
