| 彭涛,吴文能.化学通报,2021,84(6):604-609. |
| 含4(3H)-喹唑啉酮结构的取代1,3,4-噁二唑(噻二唑)化合物的合成及抗菌活性研究 |
| Syntheses and Antifungal Activities of 1, 3, 4-Oxadiazole (Thiadiazole) Derivatives Containing 4(3H)-Quinazolinone Moiety |
| 投稿时间：2020-12-04 修订日期：2020-12-21 |
| DOI： |
| 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:Quinazolinone 1,3,4-Oxadiazole 1,3,4-Thiadiazole Antibacterial 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 |
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| 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. |
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