首页|新型酰基磺酰亚胺类化合物的合成及生物活性

新型酰基磺酰亚胺类化合物的合成及生物活性

扫码查看
以邻苯二甲酸酐、磺胺和氯甲酸丁酯为原料,通过活性亚结构拼接合成了一个系列20 个新型酰基磺酰亚胺类衍生物 3a~3t,其结构均经过了1H NMR、13C NMR 和高分辨质谱确证。分别采用菌丝生长速率法和茎叶喷雾法测定了目标化合物的抑菌活性和除草活性。抑菌活性测定结果显示:在 50 mg/L下,大部分化合物对油菜菌核病菌、茶叶炭疽病菌、白芨白绢病菌和辣椒疫霉具有较好的抑制作用;化合物 3f、3n和 3q对油菜菌核病菌的抑制率分别为63。98%、79。56%和 77。83%,优于对照药剂磺草灵(58。78%);化合物 3q对油菜菌核病菌、茶叶炭疽病菌的EC50 值分别为 10。49 mg/L和 21。57 mg/L,优于磺草灵。除草活性测定结果显示,在 150 mg/L 时,化合物 3a对稗草的鲜重防效为 52。48%,低于磺草灵(71。68%)。本研究所合成的新型酰基磺酰亚胺类新化合物具有较好的抑菌活性,可为新型酰基磺酰亚胺衍生物的抑菌活性研究提供参考。
Synthesis and bioactivity of novel sulfonazoline analogues
A series of 20 novel acylsulfonimide derivatives 3a-3t were synthesized from phthalic anhydride,sulfonamide and butyl chloroformate by means of active substructure splicing.Their structures were confirmed by 1H NMR,13C NMR and high resolution mass spectrometry.The fungicidal and herbicidal activities of the target compounds were determined using the mycelial growth rate method and the stem and leaf spray method,respectively.The results of fungicidal activity showed that most of the compounds had good inhibitory effects against Sclerotinia sclerotiorum,Colletotrichum camalliae,Sclerotium rolfii and Phytophthora capsici at 50 mg/L.The inhibition rates of 3f,3n and 3q against S.sclerotiorum were 63.98%,79.56%and 77.83%,respectively,which were better than that of the commercial asulox(58.78%).The EC50 values of compound 3q against C.camalliae and S.sclerotiorum were 21.57 mg/L and 10.49 mg/L,respectively,which were better than asulox.The herbicidal activity results showed that,the fresh weight control effect of compound 3a against Echinochloa crus-galli was 52.48%at 150 mg/L,which was lower than asulox(71.68%).The novel compounds synthesized in this study displayed fungicidal activities,which can provide reference for the study of biological activities of novel acyl sulfonimide derivatives.

acylsulfonimides compoundscarbamatefungicidal activityherbicidal activity

李瑞丽、徐志红、周静、杜晓英、朱祥

展开 >

长江大学 农学院,湖北 荆州 434025

长江大学 农药研究所,湖北 荆州 434025

酰基磺酰亚胺类化合物 氨基甲酸酯 抑菌活性 除草活性

中国博士后科学基金国家自然科学基金湖北省自然科学基金湖北省教育厅基金

2022M710917323024172023AFB287B2021051

2024

农药学学报
中国农业大学

农药学学报

CSTPCD北大核心
影响因子:0.879
ISSN:1008-7303
年,卷(期):2024.26(1)
  • 17