农药学学报2016，Vol.18Issue(6)：686-696,11.DOI:10.16801/j.issn.1008-7303.2016.0096
新型4（3H）-喹唑啉酮席夫碱衍生物的合成及抗烟草花叶病毒活性
Synthesis and anti-TMV activity of novel 4(3H)-quinazolinone derivatives containing a Schiff base moiety
摘要
Abstract
A series of 4(3H)-quinazolinone derivatives containing a Schiff base moiety were synthesized and their antiviral activity against tobacco mosaic virus (TMV) was evaluated using half-leaf methodin vivo. Bioactivity results exhibited that the target compounds3a-3x under 500 μg/mL displayed moderate to good anti-TMV activities with the curative activity, protection activity, and inactivation activity values of 40.4%-53.1%, 51.2%-72.6%, and 46.0%-90.7%, respectively. Especially, compound3d showed excellent protection activity against TMV, with a half-maximal effective concentration (EC50) value of 203.89 μg/mL, which was even superior to that of ningnanmycin (214.90μg/mL). SAR analysis showed that compounds with electron-withdrawing groups at R1 and R2 positions displayed better anti-TMV activity. These results indicated that the series of 4(3H)-quinazolinone derivatives containing a Schiff base moiety can effectively control TMV.关键词
4(3H)-喹唑啉酮/席夫碱/合成/抗烟草花叶病毒活性Key words
4(H)-quinazolinone/Schiff base/synthesis/anti-TMV activity分类
化学化工引用本文复制引用
王翔,蒋向辉,汤承浩,韦国兰..新型4（3H）-喹唑啉酮席夫碱衍生物的合成及抗烟草花叶病毒活性[J].农药学学报,2016,18(6):686-696,11.基金项目
Fond project:Guizhou Province Natural Science United Fund (No. JLKK [2013]03 and LH [2015]7740) and Guizhou Province Education Quality Promotion Engineering Project (No. KY [2014]228) （No. JLKK [2013]03 and LH [2015]7740）
