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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

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【作者】 王琴张燕饶念李丹鄢龙家乐意刘力

【Author】 WANG Qin;ZHANG Yan;RAO Nian;LI Dan;YAN Long-jia;LE Yi;LIU Li;School of Pharmacetutical Sciences, Guizhou University;Guizhou Synthetic Drugs of Guizhou Province;

【通讯作者】 乐意;刘力;

【机构】 贵州大学药学院贵州省合成药物工程实验室

【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1H NMR、13C 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EC50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

【Abstract】 Twenty-three quinazolinones containing amide units were designed and synthesized.Their structures were confirmed by 1H NMR,13C NMR,and HRMS.All these compounds were evaluated for antibacterial activities against Xanthomonas oryzae(Xoo),Pseudomonas syringae(Psa)and Xanthomonas axonopodis(Xac)at 100 μg·mL-1 and 50 μg·mL-1 respectively.The results indicated that these compounds performed well activities against Xac.The EC50 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(4 i)showed much higher antibacterial activity against Xac than positive control, which was reached to 8.98 μg·mL-1.

【关键词】 酰胺喹唑啉酮合成抗菌活性
【Key words】 amide moietyquinazolonesynthesisantimicrobial activity
【基金】 贵州省科技计划项目(黔科合基础[2020]1Y109)资助
  • 【文献出处】 化学研究与应用 ,Chemical Research and Application , 编辑部邮箱 ,2022年03期
  • 【分类号】TQ455.4
  • 【下载频次】502
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