In search of novel potent bioactive compounds, a series of novel maleimide-based thiourea
derivatives containing terpinene structure were designed and synthesized. Their structures were characterized
by IR, MS, NMR, UV-vis and elemental analysis. The preliminary bioassay showed that the
target compounds exhibited a certain fungicidal activity, in which compound 2-methoxyphenyl-Naminoethyl-
terpinene-maleimide-based thiourea 5h exhibited the best inhibitory ratio of 64.2%
against Alternaria solani at the concentration of 50 μg•mL-1. A few of the target compounds showed a certain growth inhibition
activity against rape root (Brassica campestris), in which compound 5h exhibited the best inhibitory ratio of
82.0% (A-class activity level) at the concentration of 100 μg•mL-1. The intermediate 4 exhibited excellent growth inhibitory
ratio of 92.3% (A-class activity level) against rape root at the concentration of 100 μg•mL-1. In addition, the structureantifungal
activity relationship of these compounds was also discussed.
为了寻找新型强效
生物活性化合物,我们设计并合成了一系列含有
萜品烯结构的新型马来
酰亚胺基
硫脲衍
生物。通过红外光谱、质谱、核磁共振、紫外-可见光谱和元素分析对它们的结构进行了表征。初步
生物测定表明,目标化合物具有一定的杀菌活性,其中 2-
甲氧基苯基-Naminoethyl-萜烯-马来
酰亚胺基
硫脲 5h 化合物在 50 μg-mL-1 浓度下对交替孢属 solani 的抑制率最高,达到 64.2%。少数目标化合物对油菜根(Brassica campestris)表现出一定的生长抑制活性,其中化合物 5h 在 100 μg-mL-1 浓度下表现出 82.0% 的最佳抑制比(A 级活性
水平)。中间体 4 在 100 μg-mL-1 浓度下对油菜根的生长抑制率为 92.3%(A 级活性
水平),表现优异。此外,还讨论了这些化合物的结构与真菌活性的关系。