吡啶联喹唑啉酮衍生物的设计、合成与抗菌活性研究  

Design,synthesis and antibacterial activity of pyridylquinazolone derivatives

作　　者：乐意[1,2] 陈冬梅 陈玉梅 杨致松 鄢龙家 欧阳贵平 LE Yi;CHEN Dong-mei;CHEN Yu-mei;YANG Zhi-song;YAN Long-jia;OUYANG Gui-ping(School of Pharmacetutical Sciences,Guizhou University,Guiyang 550025,China;Guizhou Synthetic Drugs of Guizhou Province,Guiyang 550025,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025 [2]贵州省合成药物工程实验室,贵州贵阳550025

出　　处：《化学研究与应用》2021年第4期652-658,共7页Chemical Research and Application

基　　金：贵州省科技计划项目(黔科合基础[2020]1Y109)资助。

摘　　要：以靛红酸酐为起始原料,设计并合成了14个结构新颖的吡啶联喹唑啉酮类衍生物。所有化合物经1H NMR、13 C NMR和高分辨质谱(HRMS)表征确证其结构。初步抗菌活性结果显示,该类化合物对水稻白叶枯病菌(Xanthomonas oryzae pv.Oryzae,Xoo)、猕猴桃溃疡病菌(Pseudomonassyringae pv.actinidae,Psa)和玉米纹枯病菌(Rhizoctonia solani,Rs)均表现出一定的抑制活性。其中化合物2-([3,3′-联吡啶]-5-基)-6-氯-3,8-二甲基喹唑啉-4(3 H)-酮(3m)对Rs的抑制活性可达(51.8%)。Fourteen pyridylquinazolone derivatives with novel structures were designed and synthesized from indic anhydride.Their structures were confirmed by 1H NMR,13 C NMR and high resolution mass spectrometry(HRMS).The preliminary results showed that these compounds had certain inhibitory activities against Xanthomonas oryzae pv.Oryzae(Xoo),Pseudomonas syringae pv.Actinidae(Psa)and Rhizoctonia solani(Rs).The inhibitory activity of compound 3m against Rs was 51.8%.

关 键 词：吡啶 喹唑啉酮 合成 抑菌活性 

分 类 号：O621[理学—有机化学]