| 含不同芳香取代基的肼基二硫代甲酸甲酯-Ga3+配合物的合成及抑菌活性 |
| Synthesis and Antibacterial Activity of Gallium Complexes of Methyl Hydrazinecarbodithioate Bearing Different Aromatic Substituents |
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| 摘要: 设计合成了4种含不同芳香取代基团的肼基二硫代甲酸甲酯配体(2-乙酰基吡啶肼基二硫代甲酸甲酯(L1-H)、2-甲酰基吡啶肼基二硫代甲酸甲酯(L2-H)、2-甲酰基噻吩肼基二硫代甲酸甲酯(L3-H)、2-甲酰基水杨醛肼基二硫代甲酸甲酯(L4-H))的镓配合物, 对它们的抑菌活性进行了测试, 并讨论了配体分子中不同芳香取代基对配合物抑菌活性的影响.在模拟生理条件下, L-H与Ga3+生成较稳定的单核配合物[Ga(L1)2]NO3 (1)、[Ga(L2)2]NO3 (2)、[Ga(L3)2]NO3 (3)、[Ga(L4)2]NO3 (4),各配合物对金黄色葡萄球菌和大肠杆菌表现出比Ga(NO3)3·9H2O强的抑制活性, 抑制金黄色葡萄球菌的能力高于大肠杆菌, 其中, 1和2的活性比相应配体高, 其余2个配合物与其配体之间无明显活性差异.L1-H和L2-H分子中吡啶基的较强吸电子效应可能是1和2具有较强抑菌活性的主要原因.4种配合物抑制黑曲霉生长的活性同样高于Ga(NO3)3·9H2O,其中3最强, 并显着高于L3-H,其余配合物与相应配体间无活性差异. |
| 关键词: 镓配合物 肼基二硫代甲酸甲酯衍生物 抗菌活性 构效关系 |
| 基金项目: 江苏省自然科学基金(No.BK2012674),江苏省新型环保重点实验室开放基金(No.AE201029)资助项目. |
| Abstract: Four methyl hydrazinecarbodithioate derivatives containing different aromatic substituents including S-methyl-N'-(1-pyridin-2-yl-ethylidene)-hydrazinecarbodithioate (L1-H), S-methyl-N'-(1-pyridin-2-yl-methylene)-hydrazinecarbodithioate (L2-H), S-methyl-N'-(1-thiophen-2-yl-methylene)-hydrazinecarbodithioate (L3-H), S-methyl-2-hydroxyl benzylidenehydrazinecarbodithioate (L4-H), and their gallium complexes were synthesized and structurally characterized. Their antibacterial activities were tested using Staphylococcus aureus and Escherichia coli as substrates. The effect of different aryl substituents of ligands on the activities of each complex was studied. The results show that the four ligands can bind with Ga3+ forming mononuclear complexes, [Ga(L1)2]NO3 (1), [Ga(L2)2]NO3 (2), [Ga(L3)2]NO3 (3), [Ga(L4)2]NO3 (4), respectively, and each complex is stable under near physiological conditions. The antibacterial activities of the complexes and corresponding ligands for both bacterial are higher than Ga(NO3)3·H2O, and the inhibitory efficacy for Staphylococcus aureus is higher than that for Escherichia coli. Among the complexes, the activities of both complex 1 and complex 2 are more potent than corresponding ligand but the other two didn't show significant difference in activity. The electro-withdrawing effect of pyridyl on L1-H and L2-H may be responsible for the higher activity of complexes 1 and 2. The inhibitory activities of four complexes for Aspergillus niger are likewise more potent than Ga(NO3)3·9H2O. The complex 3 is among the most potent and its activity is higher than L3-H. Little activity difference between the other complexes was observed. |
| Keywords: gallium(Ⅲ) complex methyl hydrazinecarbodithioate antibacterial activity structure-activity relationship |
| 投稿时间：2014-04-11 修订日期：2014-06-04 |
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| 徐保莲,代坤,陈景文.含不同芳香取代基的肼基二硫代甲酸甲酯-Ga3+配合物的合成及抑菌活性[J].无机化学学报,2014,30(12):2733-2739. |
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| Support information: 相关附件： file140231 Supporting Information.pdf |
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