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金属抗生素:头孢唑林的钴(II)、铜(II)、镍(II)和锌(II)配合物的合成及抗菌活性

Metalloantibiotics: synthesis and antibacterial activity of cobalt(II), copper(II), nickel(II) and zinc(II) complexes of kefzol.

作者信息

Chohan Zahid H, Supuran Claudiu T, Scozzafava Andrea

机构信息

Department of Chemistry, Bahauddin Zakariya University, Multan, Pakistan.

出版信息

J Enzyme Inhib Med Chem. 2004 Feb;19(1):79-84. doi: 10.1080/14756360310001624939.

Abstract

Kefzol (kzl), a beta-lactam antibiotic, possesses various donor sites for interaction with transition metal(II) ions [Co(II), Cu(II), Ni(II) and Zn(II)] to form complexes of the type [M(kzl)2]Cl2 and [M(kzl)Cl], with molar ratio of metal: ligand (M:L) of 1:2 and 1:1 respectively. These complexes were prepared and characterized by physicochemical and spectroscopic methods. Their IR and NMR spectra suggest that kefzol potentially acts as a bidentate, tridentate as well as monoanionic tetradentate ligand. The complexes have been screened for antibacterial activity and results were compared with the activity of the uncomplexed antibiotic against Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli and Proteus mirabilis. The metal complexes were found to be more potent against one or more bacterial species than the uncomplexed kefzol.

摘要

头孢唑林(kzl),一种β-内酰胺抗生素,具有多个供体位点,可与过渡金属(II)离子[钴(II)、铜(II)、镍(II)和锌(II)]相互作用,形成[M(kzl)2]Cl2和[M(kzl)Cl]类型的配合物,金属与配体(M:L)的摩尔比分别为1:2和1:1。通过物理化学和光谱方法制备并表征了这些配合物。它们的红外光谱和核磁共振光谱表明,头孢唑林可能作为双齿、三齿以及单阴离子四齿配体。对这些配合物进行了抗菌活性筛选,并将结果与未配合的抗生素对金黄色葡萄球菌、肺炎克雷伯菌、铜绿假单胞菌、大肠杆菌和奇异变形杆菌的活性进行了比较。发现金属配合物对一种或多种细菌的活性比未配合的头孢唑林更强。

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