State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd., Shenyang 110021, China.
J Agric Food Chem. 2014 Dec 31;62(52):12491-6. doi: 10.1021/jf504018z. Epub 2014 Dec 19.
A series of novel substituted 3-(pyridin-2-yl)benzenesulfonamide derivatives were designed and synthesized using 2-phenylpridines as the lead compound by intermediate derivatization methods in an attempt to obtain novel compound candidates for weed control. The herbicidal activity assay in glasshouse tests showed several compounds (II6, II7, II8, II9, II10, II11, III2, III3, III4, and III5) could efficiently control velvet leaf, youth-and-old age, barnyard grass, and foxtail at the 37.5 g/ha active substance. Especially, the activities of II6, II7, III2, and III4 were proved roughly equivalent to the saflufenacil and better than 95% sulcotrione at the same concentration. The result of the herbicidal activity assay in field tests demonstrated that II7 at 60 g/ha active substance could give the same effect as bentazon at 1440 g/ha active substance to control dayflower and nightshade, meanwhile II7 showed better activity than oxyfluorfen to control arrowhead and security to rice. The present work indicates that II7 may be a novel compound candidate for potential herbicide.
设计并合成了一系列新型取代的 3-(吡啶-2-基)苯磺酰胺衍生物，以 2-苯基吡啶为先导化合物，通过中间体衍生化方法进行合成，旨在获得新型的除草化合物候选物。温室试验中的除草活性测定表明，几种化合物（II6、II7、II8、II9、II10、II11、III2、III3、III4 和 III5）能够以 37.5 g/ha 有效成分有效防治苘麻、马齿苋、稗草和狗尾草。特别是，II6、II7、III2 和 III4 的活性与 saflufenacil 相当，在相同浓度下优于 95%磺草酮。田间试验中的除草活性测定结果表明，以 60 g/ha 有效成分的 II7 可以达到与 1440 g/ha 有效成分的苯达松相同的防治效果，同时 II7 对空心菜和茄子的防治效果优于草甘膦，对水稻的安全性优于草甘膦。本工作表明，II7 可能是一种具有潜在除草活性的新型化合物候选物。
