摘要/Abstract
水稻纹枯病是水稻的三大病害之一，发病后可造成水稻严重减产，使用杀菌剂是使水稻免遭病害侵扰的有效途径之一.由于杀菌剂使用一段时间后病菌不可避免地会对其产生抗药性，因此需要不断开发结构新颖的化合物.采用中间体衍生化方法，设计并合成了25个结构新颖的苯基吡唑氧基丙酸衍生物.所有化合物都进行了离体生物活性测试，并讨论了构效关系.生物活性测试数据表明，结构新颖的苯基吡唑氧基丙酸衍生物对水稻纹枯病菌均具有良好的抑制作用，其中2-（（1-（4-氯苯基）-1H-吡唑-3-基）氧基）-N-（4-硝基苯基）丙酰胺（17）（EC50=1.05 mg/L）和2-（（1-（4-氯苯基）-1H-吡唑-3-基）氧基）-N-（吡啶-2-基）丙酰胺（22）（EC50=1.02 mg/L）对水稻纹枯病菌的杀菌活性与对照药物戊唑醇（EC50=1.02 mg/L）相当；2-（（1-（4-氯苯基）-1H-吡唑-3-基）氧基）-N-（3，4-二氯苯基）丙酰胺（20）（EC50=0.95 mg/L）活性略优于商品化对照药剂戊唑醇（EC50=1.02 mg/L）.
关键词: 苯基吡唑氧基丙酸衍生物, 中间体衍生化, 杀菌活性, 水稻纹枯病, 构效关系
Rice sheath blight disease, one of three most important diseases in rice, can lead to crop production loss seriously. However, the application of fungicides is an effective way to prevent rice from diseases. After being used for a period of time, the plant pathogenic fungi may develop resistance to chemical fungicide, so it is necessary to discover compounds with novel structures and further to address the problem of fungicide resistance. By employing the intermediate derivatisation method (IDM), twenty-five new phenylpyrazoloxyl propionic acid derivatives were designed and synthesized. The biological activities of title compounds were tested against Rhizoctonia solani and their structure-activity relationships (SAR) were discussed as well. The preliminary bioassay results displayed that some compounds exhibited an excellent fungicidal activity against Rhizoctonia solani, especially 2-((1-(4-chlorophenyl)-1H-pyrazol-3-yl)oxy)-N-(4-nitrophenyl)propanamide (17) (EC50=1.05 mg/L) and 2-((1-(4-chlorophenyl)-1H-pyrazol-3-yl)oxy)-N-(pyridin-2-yl)propanamide (22) (EC50=1.02 mg/L) showing a com-parable activity to the commercial contrast tebuconazole (EC50=1.02 mg/L), and 2-((1-(4-chlorophenyl)-1H-pyrazol-3-yl)-oxy)-N-(3,4-dichlorophenyl)propanamide (20) (EC50=0.95 mg/L) is a little more active than tebuconazole (EC50=1.02 mg/L).
Key words: phenylpyrazoloxyl propionic acid derivatives, intermediate derivatization method, fungicidal activity, Rhizoctonia solani, structure-activity relationship
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