Synthesis, fungicidal activity and SAR of new amino acid derivatives containing substituted 1-(phenylthio)propan-2-amine moiety
作者:Lei Tian、Yang Gao、Xing-Jie Peng、Cheng Zhang、Wei-Guang Zhao、Xing-Hai Liu
DOI:10.1080/10426507.2021.2012471
日期:2022.2.1
Abstract Fifteen novel amino acid derivatives were designed and synthesized using natural amino acid L-valine and two non-natural amino acids as raw materials. Fungicidal activities of these amino acid derivatives were tested against Phytophthora capsici. Most of these compounds possessed excellent activity against Phytophthora capsici at 50 μg/mL. Interestingly, compound isopropyl ((2S)-1-((1-((4
摘要 以天然氨基酸L-缬氨酸和两种非天然氨基酸为原料,设计合成了15种新型氨基酸衍生物。测试了这些氨基酸衍生物对辣椒疫霉的杀真菌活性。这些化合物中的大多数在 50 μg/mL 时对辣椒疫霉具有优异的活性。有趣的是,化合物异丙基 ((2S)-1-((1-((4-fluorophenyl)thio)propan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)carbamate 5c (EC 50 = 0.43 μg/mL),异丙酯 ((2S)-1-((1-((3,4-二甲氧基苯基)硫代)丙-2-基)氨基)-3-甲基-1-氧代丁-2-基)氨基甲酸酯5g (EC 50 =0.49 μg/mL),异丙基((2S)-1-((1-((4-(乙炔氧基)苯基)硫基)丙-2-基)氨基)-3-甲基-1-氧代丁烷-2-基)氨基甲酸酯5h(EC 50 =0.15 μg/mL)和异丙基((2S