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Synthesis, DNA binding, and antimicrobial studies of novel metal complexes containing a pyrazolone derivative Schiff base

机译:含吡唑啉酮衍生物席夫碱的新型金属配合物的合成,DNA结合和抗菌研究

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A novel series of Co(II), Ni(II), Cu(II), Zn(II), and VO(IV) complexes has been synthesized from the Schiff base derived from 4-[(3,4-dimethoxybenzylidene)amino]-1,5-dimethy1-2-phenyl-1,2- dihydropyrazol-3-one and 1,2-diaminobenzene. Structural features were determined by analytical and spectral techniques. Binding of synthesized complexes with calf thymus DNA (CT DNA) was studied by spectroscopic methods and viscosity measurements. Experimental results indicate that the complexes are able to form adducts with DNA and to distort the double helix by changing the base stacking. Lower DNA affinity of the VO(IV) complex is caused by the change of coordination geometry by the vanadyl ion resulting in a somewhat unfavorable configuration for the DNA binding. Oxidative DNA cleavage activities of the complexes were studied with supercoiled (SC) pUC19 DNA using gel electrophoresis; the mechanism studies revealed that the hydroxyl radical is likely to be the reactive species responsible for the cleavage of pUC19 DNA by the synthesized complexes. The in vitro antimicrobial screening effects of the investigated compounds were monitored by the disc diffusion method. The synthesized Schiff base complexes exhibit higher antimicrobial activity than the respective free Schiff base.
机译:从4-[(3,4-二甲氧基亚苄基)氨基衍生的席夫碱合成了一系列新颖的Co(II),Ni(II),Cu(II),Zn(II)和VO(IV)配合物。 ] -1,5-二甲基1-2-苯基-1,2-二氢吡唑-3-酮和1,2-二氨基苯。通过分析和光谱技术确定结构特征。通过光谱方法和粘度测量研究了合成的复合物与小牛胸腺DNA(CT DNA)的结合。实验结果表明,该复合物能够与DNA形成加合物,并能够通过改变碱基堆积来扭曲双螺旋结构。 VO(IV)配合物的较低DNA亲和力是由于钒基离子配位几何形状的变化而导致,导致DNA结合的构型有些不利。使用凝胶电泳,用超螺旋(SC)pUC19 DNA研究了复合物的氧化DNA切割活性。机理研究表明,羟基自由基很可能是合成复合物裂解pUC19 DNA的反应性物种。通过圆盘扩散法监测所研究化合物的体外抗菌筛选作用。合成的席夫碱复合物比相应的游离席夫碱具有更高的抗菌活性。

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