酰腙氧钒(Ⅴ)配合物的合成、结构及其抑制幽门螺旋杆菌脲酶研究 |
Synthesis, Structures, and Helicobacter Pylori Urease Inhibition of Oxovanadium(Ⅴ) Complexes with Hydrazones |
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摘要: 为了探索新型高效脲酶抑制剂, 本文合成了2个新的酰腙氧钒(Ⅴ)配合物, [VOL1(OCH3)(CH3OH)] (1)和[VOL2(μ-OCH3)]2 (2)(H2L1=N′-(5-氯-2-羟基苯亚甲基)-3-硝基苯甲酰肼;H2L2=N′-(5-氯-2-羟基苯亚甲基)-4-氯苯甲酰肼), 并通过物理化学方法和单晶X-射线衍射表征了它们的结构。化合物1是一个单核配合物, 而化合物2是由两个甲氧基配体桥连的具有中心对称性的双核配合物。在每个配合物中, V原子都采取八面体配位构型。本文还研究了这两个配合物的热稳定性和它们对幽门螺旋杆菌脲酶的抑制活性。在浓度为100 μmol·L-1时, 配合物1和2对脲酶的抑制率分别为71.4%和73.3%, 其IC50值分别为63.6和37.7 μmol·L-1。 |
关键词: 酰腙 钒氧(Ⅴ)配合物 晶体结构 脲酶 抑制剂 |
基金项目: 国家自然科学基金(No.20901036), 辽宁省高校优秀青年人才支持计划(No.LJQ2011114)资助项目。 |
Abstract: In order to explore new and efficient urease inhibitors, two new oxovanadium(Ⅴ) complexes, [VOL1(OCH3)(CH3OH)] (1) and [VOL2(μ-OCH3)]2 (2) (H2L1=N′-(5-chloro-2-hydroxybenzylidene)-3-nitrobenzohydrazide; H2L2=N′-(5-chloro-2-hydroxybenzylidene)-4-chlorobenzohydrazide), have been synthesized and characterized by physico-chemical methods and single-crystal X-ray diffraction. Compound 1 is a mononuclear complex, and compound 2 is a bis-methanolato bridged centrosymmetric dinuclear complex. The V atom in each complex adopts an octahedral coordination. Thermal stability and urease inhibitory activities of the complexes were studied. The percent inhibition at the concentration of 100 μmol·L-1 on Helicobacter pylori urease is 71.4% for 1 and 73.3% for 2. The IC50 values for 1 and 2 are 63.6 and 37.7 μmol·L-1, respectively. CCDC: 858857, 1; and 858858, 2. |
Keywords: hydrazone oxovanadium(Ⅴ) complex crystal structure urease inhibitor |
投稿时间:2012-12-27 修订日期:2013-01-17 |
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赵月,韩笑,周晓霞,李海华,由忠录.酰腙氧钒(Ⅴ)配合物的合成、结构及其抑制幽门螺旋杆菌脲酶研究[J].无机化学学报,2013,29(4):867-874. |
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