In order to discover novel compounds with high-activity to control aphid,a series of novel（E）-β-farnesene analogues containing 1,2,3-thiadiazole were designed and synthesized,and their structures were confirmed by ...In order to discover novel compounds with high-activity to control aphid,a series of novel（E）-β-farnesene analogues containing 1,2,3-thiadiazole were designed and synthesized,and their structures were confirmed by IR,^1H NMR,^13C NMR,and HRMS（ESI）.The stability of representative compounds was studied by HPLC and -1H NMR techniques.Repellent activity results indicated that compounds 8h and 8j displayed 60.3%and 62.0%repellent rates,respectively.The aphicidal bioassay results showed that most analogues exhibited considerable aphicidal activity against Myzus persicae.Especially,analogues 81,8s and 8t exhibited high activity with LC50 values of 33.4 μg/mL,50.2 μg/mL and 61.8 μg/mL,respectively,which were higher than the lead compound（E）-β-farnesene,but lower than commercial insecticide pymetrozine with a LC50 of 7.1 μg/mL展开更多
To find new lead compounds with high biological activity,a series of novel 4-methyl-1,2,3-thiadiazole-5-carboxaldehyde benzoyl hydrazone derivatives were designed and synthesized.Their structures were confirmed by -1H...To find new lead compounds with high biological activity,a series of novel 4-methyl-1,2,3-thiadiazole-5-carboxaldehyde benzoyl hydrazone derivatives were designed and synthesized.Their structures were confirmed by -1H NMR,-（13）C NMR,IR spectrum and elemental analysis.Preliminary bioassay indicated that the title compounds exhibited moderate to strong fungicidal activity against six fungi in vitro at50 μg/mL.Moreover,some of the title compounds exhibited good curative activity against TMV in vivo at500 μg/mL.The structure-activity relationship analysis of compounds against Valsa mali showed that compounds containing halogen at the para position on phenyl exhibited the best activity.Especially compound 8k showed broad spectrum fungicidal activities against Valsa mali,Botrytis cinerea,Pythium aphamdermatum,Rhizoctonia solani,Fusarium moniliforme and Altemaria solani with the EC（50） values of8.20,24.42,15.80,40.53,41.48,and 34.16 μg/mL,respectively.展开更多
基金the financial support from the National Natural Science Foundation of China (No. 21132003)
文摘In order to discover novel compounds with high-activity to control aphid,a series of novel（E）-β-farnesene analogues containing 1,2,3-thiadiazole were designed and synthesized,and their structures were confirmed by IR,^1H NMR,^13C NMR,and HRMS（ESI）.The stability of representative compounds was studied by HPLC and -1H NMR techniques.Repellent activity results indicated that compounds 8h and 8j displayed 60.3%and 62.0%repellent rates,respectively.The aphicidal bioassay results showed that most analogues exhibited considerable aphicidal activity against Myzus persicae.Especially,analogues 81,8s and 8t exhibited high activity with LC50 values of 33.4 μg/mL,50.2 μg/mL and 61.8 μg/mL,respectively,which were higher than the lead compound（E）-β-farnesene,but lower than commercial insecticide pymetrozine with a LC50 of 7.1 μg/mL
基金financial support from the National Natural Science Foundation of China(No.21132003)
文摘To find new lead compounds with high biological activity,a series of novel 4-methyl-1,2,3-thiadiazole-5-carboxaldehyde benzoyl hydrazone derivatives were designed and synthesized.Their structures were confirmed by -1H NMR,-（13）C NMR,IR spectrum and elemental analysis.Preliminary bioassay indicated that the title compounds exhibited moderate to strong fungicidal activity against six fungi in vitro at50 μg/mL.Moreover,some of the title compounds exhibited good curative activity against TMV in vivo at500 μg/mL.The structure-activity relationship analysis of compounds against Valsa mali showed that compounds containing halogen at the para position on phenyl exhibited the best activity.Especially compound 8k showed broad spectrum fungicidal activities against Valsa mali,Botrytis cinerea,Pythium aphamdermatum,Rhizoctonia solani,Fusarium moniliforme and Altemaria solani with the EC（50） values of8.20,24.42,15.80,40.53,41.48,and 34.16 μg/mL,respectively.
