中文关键词:喹唑啉酮1，3，4-噁二唑1，3，4-噻二唑抗菌活性 英文关键词:Quinazolinone1,3,4-Oxadiazole1,3,4-ThiadiazoleAntibacterial activity 基金项目:贵州省自然科学基金项目重点项目（黔科合基础[2020]1Z023）、贵州省教育厅青年科技人才成长项目（黔教合KY字[2018]450）和贵州省生物制药工程研究中心项目（黔教合KY字[2019]051）资助

作者	单位	E-mail
彭涛	茅台学院酿酒工程系 仁怀 564500
吴文能	贵阳学院食品与制药工程学院 贵阳 550005	wuwenneng123@126.com

摘要点击次数:324 全文下载次数:0 中文摘要: 以2-氨基苯甲酸为原料，通过环化、缩合、肼解、环化、硫醚化和氧化等步骤，合成了10个含喹唑啉酮取代1，3，4-噁二唑（噻二唑）化合物。通过¹H NMR、¹³C NMR、MS和元素分析进行确证其结构。初步抑菌活性测试表明，化合物浓度在50μg/mL时对葡萄座腔菌（Botryosphaeria dothidea）、拟茎点霉菌（Phomopsis sp.）和灰霉菌（B. cinerea）具有中等抑制活性。另外，目标化合物对猕猴桃溃疡病（Pseudomonas syringae pv. actinidia）均具有一定的抑制活性，其中，化合物6a和6b对猕猴桃溃疡病的EC₅₀值为11.7和20.5 μg/mL，优于对照药剂叶枯唑（24.5μg/mL）。这类化合物具有较好抗菌的生物活性，在此基础上进行结构优化有望发现较高活性化合物。 英文摘要: Using 2-aminobenzoic acid as raw material, ten 1,3,4-oxadiazole (thiadiazole) compounds containing quinazolin-4(3H)-one were synthesized through five step reactions including cyclization, condensation, hydrazinolysis, cyclization, thioetherification and oxidation. The structures of titled compounds were characterized by ¹H NMR, ¹³C NMR, MS and elemental analysis. The preliminary antifungal activity test indicated that the target compounds have moderate inhibitory activity against Botryosphaeria dothidea, Phomopsis sp. and B. cinerea at the concentration of 50μg/mL. The target compounds have good inhibitory activity against Pseudomonas syringae pv. actinidia, and the EC₅₀ values of compounds 6a and 6b against Pseudomonas syringae pv. actinidia are 11.7μg/mL and 20.5μg/mL, which are better than the control agent Bismerthiazol (24.5μg/mL). This kind of compounds have good biological activity for antibacterial. On this basis, the structure optimization is expected to find a compound with higher activity. 查看全文查看/发表评论下载PDF阅读器 相关附件：附件1版权转让声明书 -->