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酰胺类化合物的合成及杀菌活性研究

Synthesis of amide compounds and determination of bactericidal activity
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摘要 植物杀菌剂的施用是保障粮食安全的重要手段。然而,随着杀菌剂的持续使用,真菌的耐药性也在逐渐增强。为缓解真菌耐药性问题,开发新型杀菌剂,本试验设计合成了13个酰胺类化合物L1-L13,采用菌丝生长速率法对目标化合物进行离体活性评价,结果表明在100μg/mL的浓度下,化合物L1、L2、L4、L6和L9对黄瓜灰霉菌(Botrytis cinerea)的抑制率均为100%,与阳性对照药剂吡唑醚菌酯效果相当(P>0.05),然后对这几种化合物进行EC_(50)值的测定,化合物L2和L4对黄瓜灰霉菌的EC_(50)值分别为1.424和0.673μg/mL,优于阳性对照药剂吡唑醚菌酯4.009μg/mL(P<0.05)。还测定了化合物L2和L4对黄瓜灰霉菌的活体防治EC_(50)值,化合物L2和L4的活体防治EC_(50)值分别为1.060和0.660μg/mL,防治效果良好。表明本研究发现的目标化合物可作为新型杀菌剂候选化合物,可用于后续应用研究。 The application of plant fungicides is an important means to ensure food security.However,with the continuous use of fungicides,the resistance of fungi is gradually increasing.To alleviate the problem of fungal resistance and develop new fungicides,13 amide compounds L1L13 were designed and synthesized in this paper.The in vitro activity of the target compounds was evaluated by the mycelial growth rate method.At a concentration of 100µg/mL,the inhibition rates of compounds L1,L2,L4,L6 and L9 against Botrytis cinerea on cucumber were all 100%,which were comparable to the positive control fungicide pyraclostrobin(P>0.05).Then,the EC_(50) values of the compounds were determined.The EC_(50) values of compounds L2 and L4 against Botrytis cinerea on cucumber were 1.424 and 0.673µg/mL,respectively,which were better than the positive control fungicide pyraclostrobin 4.009µg/mL(P<0.05).The EC_(50) values of compounds L2 and L4 for the in vivo control of Botrytis cinerea on cucumber were determined as 1.060 and 0.660µg/mL,respectively,which suggested a good control effects.The results suggested that the target compounds discovered in this study can be used as candidate compounds for new fungicides and can be applied in subsequent research.
作者 栗猛超 王正忠 孙素素 张金林 LI Mengchao;WANG Zhengzhong;SUN Susu;ZHANG Jinlin(College of Plant Protection,Hebei Agricultural University,Baoding 071001,China)
出处 《河北农业大学学报》 北大核心 2025年第6期63-69,共7页 Journal of Hebei Agricultural University
基金 国家自然科学基金项目(32272573)。
关键词 酰胺类化合物 设计 化学合成 杀菌活性 amide compounds design chemical synthesis antifungal activity
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