Design, synthesis and herbicidal activities of novel 4-(1H-pyrazol-1-yl)-6-( alkynyloxy)pyrimidine derivatives as potential pigment biosynthesis inhibitors
Design, synthesis and herbicidal activities of novel 4-(1H-pyrazol-1-yl)-6-( alkynyloxy)pyrimidine derivatives as potential pigment biosynthesis inhibitors
复制标题
作为潜在色素生物合成抑制剂的新型4-(1H-吡唑-1-基)-6-(炔氧基)嘧啶衍生物的设计、合成及其除草活性
DOI：
10.1002/ps.3633
复制
发表时间：
2014-06-01
影响因子：
4.1
通讯作者：
Li, Jian-Hong
中科院分区：
文献类型：
--
作者：
Ma, Hong-Ju;Zhang, Jian-Hua;Li, Jian-Hong
为了寻找新的有价值的除草剂候选物，合成了一系列新的4-（1h -吡唑-1-酰基）-6-（烷基氧基）-嘧啶衍生物，并对其进行了体内除草活性评价。结果许多目标化合物表达漂白活性。其中，化合物5h对禾本科杂草的漂白活性最好，对狼尾草（Pennisetum alopecuroides L.）幼苗叶绿素水平的抑制作用最高（IC50 = 3.48mg L-1）。化合物5h在禾本科植物P. alopecuroides L.和阔叶植物Brassica campestris L.之间表现出良好的选择性毒性。结论含吡唑的嘧啶类衍生物可作为开发新型色素生物合成抑制剂的先导化合物。(c) 2013年化学工业学会
BACKGROUNDWith the objective of finding novel valuable herbicidal candidates, a series of novel 4-(1H-pyrazol-1-yl)-6-(alkynyloxy)-pyrimidine derivatives were synthesised and their herbicide activities were evaluated in vivo.RESULTSThe results showed that many target compounds expressed bleaching activities. Among these, compound 5h showed the best bleaching activity to gramineous weeds, being able to produce the highest inhibition of chlorophyll level in seedlings of Pennisetum alopecuroides L. (IC50 = 3.48mg L-1). Moreover, compound 5h expressed good selective toxicity between gramineous P. alopecuroides L. and broadleaf plant Brassica campestris L.CONCLUSIONSThe present work demonstrates that pyrimidine derivatives containing pyrazole can be used as potential lead compounds for developing novel pigment biosynthesis inhibitors. (c) 2013 Society of Chemical Industry