| 新型4(3H)-喹唑啉酮席夫碱衍生物的合成及抗烟草花叶病毒活性 |
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| 引用本文： | 王翔,蒋向辉,汤承浩,韦国兰.新型4(3H)-喹唑啉酮席夫碱衍生物的合成及抗烟草花叶病毒活性[J].农药学学报,2016,18(6):686-696. |
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| 作者姓名： | 王翔 蒋向辉 汤承浩 韦国兰 |
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| 作者单位： | 1.凯里学院, 黔东南民族药综合利用工程技术研究中心, 贵州 凯里 556011 |
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| 摘 要： | 合成了一系列含席夫碱的4（3H）-喹唑啉酮衍生物，并采用半叶枯斑法测试了目标化合物抗烟草花叶病毒活性。结果表明:目标化合物在500 μg/mL下对烟草花叶病毒的治疗活性为40.4%~53.1%，保护活性为51.2%~72.6%，钝化活性为46.0%~90.7%，其中，化合物3d的保护活性较好，有效抑制中浓度（EC50）值为203.89 μg/mL，略优于商业化抗病毒剂宁南霉素（EC50值214.90 μg/mL）。初步构效关系结果表明:在苯环的R1及R2位上引入吸电子基团有利于活性的提高。本研究结果表明，含席夫碱的4（3H）-喹唑啉酮衍生物能较好地控制烟草花叶病毒。
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| 关 键 词： | 4(3H)-喹唑啉酮 席夫碱 合成 抗烟草花叶病毒活性 |
| 收稿时间： | 2016/9/16 0:00:00 |
| 修稿时间： | 2016/10/31 0:00:00 |
Synthesis and anti-TMV activity of novel 4(3H)-quinazolinone derivatives containing a Schiff base moiety |
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| WANG Xiang,JIANG Xianghui,TANG Chenghao and WEI Guolan.Synthesis and anti-TMV activity of novel 4(3H)-quinazolinone derivatives containing a Schiff base moiety[J].Chinese Journal of Pesticide Science,2016,18(6):686-696. |
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| Authors: | WANG Xiang JIANG Xianghui TANG Chenghao and WEI Guolan |
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| Institution: | 1.Qiandongnan Engineering and Technology Research Center for Comprehensive Utilization of National Medicine, Kaili University, Kaili 556011, Guizhou Province, China2.College of Chemistry and Materials Engineering, Kaili University, Kaili 556011, Guizhou Province, China |
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| Abstract: | A series of 4(3H)-quinazolinone derivatives containing a Schiff base moiety were synthesized and their antiviral activity against tobacco mosaic virus (TMV) was evaluated using half-leaf methodin vivo. Bioactivity results exhibited that the target compounds3a-3x under 500 μg/mL displayed moderate to good anti-TMV activities with the curative activity, protection activity, and inactivation activity values of 40.4%-53.1%, 51.2%-72.6%, and 46.0%-90.7%, respectively. Especially, compound3d showed excellent protection activity against TMV, with a half-maximal effective concentration (EC50) value of 203.89 μg/mL, which was even superior to that of ningnanmycin (214.90μg/mL). SAR analysis showed that compounds with electron-withdrawing groups at R1 and R2 positions displayed better anti-TMV activity. These results indicated that the series of 4(3H)-quinazolinone derivatives containing a Schiff base moiety can effectively control TMV. |
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| Keywords: | 4(H)-quinazolinone Schiff base synthesis anti-TMV activity |
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