高等学校化学学报
高等學校化學學報
고등학교화학학보
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES
2014年
8期
1703-1709
,共7页
杨冬燕%王蕾%贾长青%李长胜%马永强%芮昌辉%徐彦军%覃兆海
楊鼕燕%王蕾%賈長青%李長勝%馬永彊%芮昌輝%徐彥軍%覃兆海
양동연%왕뢰%가장청%리장성%마영강%예창휘%서언군%담조해
芳亚甲基硝基缩氨基胍%蚜虫%杀虫活性
芳亞甲基硝基縮氨基胍%蚜蟲%殺蟲活性
방아갑기초기축안기고%아충%살충활성
Arylideneamino guanidine derivative%Aphid%Insecticidal activity
依据活性亚结构拼接原理,以硝基胍为原料,合成了一系列具有新烟碱类和缩氨基脲类杀虫剂共同结构特征的芳亚甲基硝基缩氨基胍类化合物,其结构通过1 H NMR、IR和元素分析等方法进行了确证.杀虫活性测定结果表明,在600μg/mL浓度下,目标化合物对桃蚜[ Myzuspersicae( Sulzer)]具有较优异的活性,其中化合物4-2,4-8,4-10,4-16,4-27,4-31和4-34的校正死亡率均在90%以上.进一步以桃蚜、棉蚜( Aphis gossypii)和桃粉蚜(Hyalopterusamygdali blanchard)为对象,测定了化合物4-2,4-8和4-34的精密毒力.结果表明,它们在低浓度下仍然具有很高的活性,其中化合物4-8对棉蚜的活性甚至优于对照药剂吡虫啉,在3.13μg/mL浓度下致死率仍高达95.7%(吡虫啉为79.4%),具有进一步研究开发的价值.
依據活性亞結構拼接原理,以硝基胍為原料,閤成瞭一繫列具有新煙堿類和縮氨基脲類殺蟲劑共同結構特徵的芳亞甲基硝基縮氨基胍類化閤物,其結構通過1 H NMR、IR和元素分析等方法進行瞭確證.殺蟲活性測定結果錶明,在600μg/mL濃度下,目標化閤物對桃蚜[ Myzuspersicae( Sulzer)]具有較優異的活性,其中化閤物4-2,4-8,4-10,4-16,4-27,4-31和4-34的校正死亡率均在90%以上.進一步以桃蚜、棉蚜( Aphis gossypii)和桃粉蚜(Hyalopterusamygdali blanchard)為對象,測定瞭化閤物4-2,4-8和4-34的精密毒力.結果錶明,它們在低濃度下仍然具有很高的活性,其中化閤物4-8對棉蚜的活性甚至優于對照藥劑吡蟲啉,在3.13μg/mL濃度下緻死率仍高達95.7%(吡蟲啉為79.4%),具有進一步研究開髮的價值.
의거활성아결구병접원리,이초기고위원료,합성료일계렬구유신연감류화축안기뇨류살충제공동결구특정적방아갑기초기축안기고류화합물,기결구통과1 H NMR、IR화원소분석등방법진행료학증.살충활성측정결과표명,재600μg/mL농도하,목표화합물대도아[ Myzuspersicae( Sulzer)]구유교우이적활성,기중화합물4-2,4-8,4-10,4-16,4-27,4-31화4-34적교정사망솔균재90%이상.진일보이도아、면아( Aphis gossypii)화도분아(Hyalopterusamygdali blanchard)위대상,측정료화합물4-2,4-8화4-34적정밀독력.결과표명,타문재저농도하잉연구유흔고적활성,기중화합물4-8대면아적활성심지우우대조약제필충람,재3.13μg/mL농도하치사솔잉고체95.7%(필충람위79.4%),구유진일보연구개발적개치.
In order to search for better lead compounds with excellent biological activities, a novel series of acyclic neonicotinoids of nitro arylideneamino guanidine derivatives was designed and synthesized from ni-troaminoguanidine by the method of linking the active substructures of neonicotiniod insecticides and semicar-bazone insecticides. All the target compounds were confirmed by 1 H NMR, IR and elemental analysis. The preliminary bioassay showed that the lethal rates of target compounds to Myzuspersicae were excellent at the concentration of 600 μg/mL. The lethal rates of several compounds, such as 4-2, 4-8, 4-10, 4-16, 4-27, 4-31 and 4-34 , were more than 90%. Further research of compounds 4-2 , 4-8 and 4-34 against Myzuspersi-cae, Aphis gossypii and Hyalopterusamygdali blanchard indicated these compounds possessed high activity at low concentrations, especially, the activity of compound 4-8 was better than that of imidacloprid against Hya-lopteraamygdali blanchard, its lethal rate was 95.7% compared to imidacloprid(79.4%) at the concentration of 3.13 μg/mL, which confirmed that this compound is worth of research.