酰胺类喹唑啉酮衍生物的合成及抗菌活性  

Synthesis and antibacterial activity of quinazoline derivatives bearing amide moiety

作　　者：王琴 张燕 饶念 李丹 鄢龙家 乐意[1,2] 刘力 WANG Qin;ZHANG Yan;RAO Nian;LI Dan;YAN Long-jia;LE Yi;LIU Li(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》2022年第3期493-503,共11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：本文设计并合成了23个含酰胺结构单元的新型喹唑啉酮类化合物,经^(1)H NMR、^(13)C NMR和HRMS确证结构。在100μg·mL^(-1)和50μg·mL^(-1)浓度下,评价了它们对水稻白叶枯病菌、猕猴桃溃疡病菌和柑橘溃疡病菌的抑菌活性。结果表明,化合物对柑橘溃疡病菌有较强的抑制活性,并测定了6个化合物对柑橘溃疡病菌的EC_(50)值。其中,活性最优化合物1-(4-氟苯基)-3-(4-((3-甲基-4-氧代-3,4-二氢喹唑啉-2-基)甲氧基)苯基)尿素(4i)对柑橘溃疡病菌的抑菌活性优于阳性对照,达到8.98μg·mL^(-1)。Twenty-three quinazolinones containing amide units were designed and synthesized.Their structures were confirmed by^(1)H NMR,^(13)C NMR,and HRMS.All these compounds were evaluated for antibacterial activities against Xanthomonas oryzae(Xoo),Pseudomonas syringae(Psa)and Xanthomonas axonopodis(Xac)at 100μg·mL^(-1)and 50μg·mL^(-1)respectively.The results indicated that these compounds performed well activities against Xac.The EC_(50) values of the best six compounds against Xac were tested.In particular,1-(4-fluorophenyl)-3-(4-((3-methyl-4-oxo-3,4-dhydroquinazolin-2-yl)methoxy)phenyl)urea(4i)showed much higher antibacterial activity against Xac than positive control,which was reached to 8.98μg·mL^(-1).

关 键 词：酰胺 喹唑啉酮 合成 抗菌活性 

分 类 号：O621[理学—有机化学]