Design, synthesis and effect of the introduction of a propargyloxy group on the fungicidal activities of 1-substituted phenoxypropan-2-amino valinamide carbamate derivatives
作者:Jian-Qiang Li、Zhi-Peng Wang、Yang Gao、Wei-Guang Zhao
DOI:10.1039/c6ra17908h
日期:——
introduction of an additional OCH2 linker. The bioassay results indicated that compounds containing a small group at the para-position of phenyl gave excellent fungicidal activities with EC50 values ranging from 0.59 to 2.06 μmol L−1. Most notably, the introduction of a propargyloxy group led to a pronounced increase in the fungicidal activity. Furthermore, compound 7o bearing a propargyloxy group was identified
卵菌的细胞壁由纤维素组成,使纤维素合酶成为羧酸酰胺类杀菌剂的良好靶标。缬氨酰胺氨基甲酸酯是氨基酸杀真菌剂,就其减少这些化合物对人类健康和环境的不利影响的能力而言,代表了常规合成农药的极佳替代品。在继续开发新的纤维素合酶抑制剂的研究中,我们通过引入其他OCH 2接头,开发了一系列iprovalicarb的“拉伸”类似物。生物测定结果表明,在苯基对位含有少量基团的化合物具有优异的EC 50杀真菌活性。值在0.59至2.06μmolL -1之间。最值得注意的是,炔丙基氧基的引入导致杀真菌活性的显着增加。此外,带有炔丙基氧基的化合物7o被认为是最有希望的候选物,因为其对卵菌病具有优异的杀真菌效力,并且对非卵菌病具有良好的杀真菌活性。