Xie Yong, Chi Hui-Wei, Guan Ai-Ying, Liu Chang-Ling, Ma Hong-Juan, Cui Dong-Liang
State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd, Shenyang 110021, China.
State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd, Shenyang 110021, China.
Bioorg Med Chem. 2016 Feb 1;24(3):428-34. doi: 10.1016/j.bmc.2015.08.037. Epub 2015 Aug 28.
In an attempt to obtain novel candidate compound for weed control, a series of newly substituted 3-(pyridin-2-yl)benzenesulfonamide derivatives 2 were designed and synthesized using compound II7 as a lead compound by Intermediate Derivatization Methods and their herbicidal activities were evaluated. The herbicidal activity assay in greenhouse tests showed several compounds (2g, 2i, 2j, 2k, 2l, 2m, 2n and 2o) exhibited significant herbicidal activity for controlling velvet leaf (Abutilon theophrasti medic.) and youth-and-old age (Zinnia elegans jacq.) at 37.5ga.i./ha. In particular, 2h was found to be the most potential candidate herbicide and was proved higher activity than the lead compound II7. The result of the weed controlling spectrum test showed that 2h could effectively control dayflower (Commelina tuberosa), bur beggarticks (Bidens tripartita linn.), youth-and-old age, cassia tora (Cassiaobtusifolia L.), velvet leaf, purslane (Portulaca oleracea) and false daisy (Eclipta prostrata L.). In addition, the mixture of compound 2h and propanil could produce a synergistic effect and enhance herbicidal activity. The result of the herbicidal activity assay in field test demonstrated that 2h could effectively control dayflower and nightshade (Disambiguation) with long-lasting persistence. The present work indicates that 2h may be a novel compound candidate as a potential herbicide.
为了获得用于杂草防治的新型候选化合物,以化合物II7为先导化合物,采用中间体衍生化方法设计并合成了一系列新的取代3-(吡啶-2-基)苯磺酰胺衍生物2,并对其除草活性进行了评价。温室试验中的除草活性测定表明,几种化合物(2g、2i、2j、2k、2l、2m、2n和2o)在37.5ga.i./ha剂量下对控制苘麻(Abutilon theophrasti medic.)和百日草(Zinnia elegans jacq.)表现出显著的除草活性。特别是,发现2h是最具潜力的候选除草剂,并且被证明比先导化合物II7具有更高的活性。杂草防除谱试验结果表明,2h能有效防除鸭跖草(Commelina tuberosa)、鬼针草(Bidens tripartita linn.)、百日草、决明(Cassiaobtusifolia L.)、苘麻、马齿苋(Portulaca oleracea)和鳢肠(Eclipta prostrata L.)。此外,化合物2h与敌稗的混合物可产生协同效应并增强除草活性。田间试验中的除草活性测定结果表明,2h能有效防除鸭跖草和龙葵(Disambiguation),持效期长。目前的工作表明,2h可能是一种新型的潜在除草剂候选化合物。