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基于第三代氟喹诺酮类抗菌药物的混合配体 Cu(II) 配合物:结构、抗菌活性、超氧化物歧化酶活性及 DNA 相互作用研究。

Third generation fluoroquinolones antibacterial drug based mixed-ligand Cu(II) complexes: structure, antibacterial activity, superoxide dismutase activity and DNA-interaction approach.

机构信息

Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, Gujarat, India.

出版信息

J Enzyme Inhib Med Chem. 2011 Apr;26(2):188-97. doi: 10.3109/14756366.2010.487486. Epub 2010 Jun 28.

Abstract

The copper(II) complexes of the type [Cu(SPF)(A(n))Cl]/[Cu(PFL)(A(n))Cl] (where SPF is sparfloxacin, PFL is pefloxacin and A(n) is 2,2'-dipyridylamine/pyridine-2-carboxalehyde/thiophene-2-carboxaldehyde) were synthesised and were found to have a pyramidal geometry with a square base. The superoxide dismutase (SOD) like activity of the complexes were measured using an NBT/NADH/PMS system, these were expressed in terms of the concentration of complex which termianates the formation of formazan by 50% (IC₅₀ value) and found to range from 0.781 to 1.354 μM. The interactions of the complexes with DNA were studied by absorption titration, viscosity measurement and gel electrophoresis under physiological conditions. The antimicrobial efficiency of the complexes were tested on five different microorganisms and showed good biological activity.

摘要

[Cu(SPF)(A(n))Cl]/[Cu(PFL)(A(n))Cl](其中 SPF 是司帕沙星,PFL 是培氟沙星,A(n) 是 2,2'-联吡啶胺/吡啶-2-羧酸醛/噻吩-2-甲醛)类型的铜(II)配合物被合成,并被发现具有三角锥形几何形状和正方形基底。使用 NBT/NADH/PMS 系统测量了配合物的超氧化物歧化酶(SOD)样活性,并用使甲臜形成终止 50%的配合物浓度(IC₅₀ 值)来表示,发现范围从 0.781 到 1.354 μM。在生理条件下,通过吸收滴定、粘度测量和凝胶电泳研究了配合物与 DNA 的相互作用。配合物的抗菌效率在五种不同的微生物上进行了测试,表现出良好的生物活性。

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