Synthesis and Biological Activity of N-Aminoethyl-terpinene-maleimide-based Thiourea Compounds
Synthesis and Biological Activity of N-Aminoethyl-terpinene-maleimide-based Thiourea Compounds
复制标题
N-氨基乙基松油烯马来酰亚胺基硫脲化合物的合成及生物活性
DOI：
10.2174/1570178612666150226230645
复制
发表时间：
2015-01-01
影响因子：
0.8
通讯作者：
Lei, Fu-hou
中科院分区：
文献类型：
--
作者：
Liu, Lu-zhi;Liao, Jing-ni;Lei, Fu-hou
为了寻找具有生物活性的新型化合物，设计合成了一系列基于马来酰亚胺的含萜品烯结构的硫脲衍生物。其结构经IR、MS、NMR、UV-vis和元素分析表征。初步生物活性测定结果表明，目标化合物具有一定的杀菌活性，其中化合物2-甲氧基苯基-N-氨乙基-萜品烯-马来酰亚胺硫脲5 h在50 μ g·mL ~（-1）浓度下对番茄早疫病菌（Alternaria solani）的抑制率最高，为64.2%。部分目标化合物对油菜（Brassica campestris）的根生长有一定的抑制活性，其中化合物5 h在100 μ g·mL ~（-1）浓度下的抑制率最高，为82.0%（A级活性水平）。中间体4在100 μ g·mL ~（-1）的浓度下对油菜根表现出92.3%（A级活性水平）的优异生长抑制率。此外，还讨论了该类化合物的结构与抗真菌活性的关系。
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-N-aminoethyl-terpinene-maleimide-based thiourea 5h exhibited the best inhibitory ratio of 64.2% against Alternaria solani at the concentration of 50 mu g.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 mu g.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 mu g.mL(-1). In addition, the structure-antifungal activity relationship of these compounds was also discussed.