Lim Hwan Jung, Lee Won Hyung, Park Seong Jun
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology (KRICT), 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, Korea.
Central Research Institute, Kyung Nong Co. Ltd., 34-14 Summeori-gil, Kyongju 38175, Kyongsangbuk-do, Korea.
Molecules. 2019 Sep 23;24(19):3451. doi: 10.3390/molecules24193451.
Novel anthranilic diamides with sulfilimidoyl and sulfoximidoyl functionalities were successfully prepared. Among newly-prepared organosulfur compounds, 3-bromo-1-(3-chloropyridin-2-yl)--(2-methyl-6-(methylcarbamoyl)-4-(methylthio)phenyl)-1-pyrazole-5-carboxamide and (,)-3-bromo-1-(3-chloropyridin-2-yl)--(2-methyl-4-(S-methyl--(2,2,2-trifluoroacetyl)sulfinimidoyl)-6-(methylcarbamoyl)phenyl)-1-pyrazole-5-carboxamide showed good levels of efficacy and a strong correlation between insecticidal activities and physical properties, respectively. In particular, available data indicated that the -trifluoroacetyl sulfilimine moiety could be an appealing structural scaffold for the discovery of a new crop-protecting agent.
成功制备了具有亚磺酰亚胺基和磺酰亚胺基官能团的新型邻氨基苯甲酰胺。在新制备的有机硫化合物中，3-溴-1-(3-氯吡啶-2-基)-N-(2-甲基-6-(甲基氨基甲酰基)-4-(甲硫基)苯基)-1-吡唑-5-甲酰胺和(±)-3-溴-1-(3-氯吡啶-2-基)-N-(2-甲基-4-(S-甲基-N-(2,2,2-三氟乙酰基)亚磺酰亚胺基)-6-(甲基氨基甲酰基)苯基)-1-吡唑-5-甲酰胺分别表现出良好的药效水平，且杀虫活性与物理性质之间存在很强的相关性。特别是，现有数据表明，N-三氟乙酰基亚磺酰亚胺部分可能是发现新型作物保护剂的一个有吸引力的结构支架。
