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依诺沙星、沙拉沙星金属配合物的合成及结构表征

发布时间:2018-08-06 12:38
【摘要】:许多药理学的研究表明:大部分具有生物活性的药物与金属形成配合物后影响药物的临床疗效;再者,喹诺酮类药物的结构上存在多个配位点,为构筑配合物体系提供了可能性;另外,其配位聚合物在医药及功能材料中具有潜在的应用前景。因此,喹诺酮类药物金属配合物的合成及性质研究在近几年来受到了极大的关注。目的:通过合成依诺沙星及沙拉沙星药物金属配合物和表征配合物的晶体结构,总结合成条件及规律,分析晶体的拓扑类型,考察分子间的作用力,研究配合物的几何构型及辅助配体对配合物的影响,探讨药物与金属的配位方式。为其它喹诺酮类药物金属配合物的合成提供参考,为进一步研究金属离子对此类药物生物活性的影响奠定理论基础,为开发新型价格低廉的喹诺酮类药物及指导临床用药提供科学依据。方法:以依诺沙星和沙拉沙星药物为主要配体,以过渡金属为配位反应中心,采用水热法合成配位化合物;利用X-射线单晶衍射技术,元素分析、红外光谱表征了配合物的晶体结构。结果:合成出符合晶体学要求的4种金属配合物,分别是依诺沙星与过渡金属锌(Ⅱ)、铜(Ⅱ)构筑的两个配合物;依诺沙星、噻吩-2,5-二羧酸与过渡金属镉构筑的配合物;沙拉沙星、对苯二甲酸与过渡金属锰(Ⅱ)构筑的配合物。结论:本论文阐述了4个由喹诺酮类药物与金属所构筑配合物的晶体结构。其中,依诺沙星-锌(Ⅱ)、铜(Ⅱ)配合物为离子型化合物;依诺沙星-噻吩-2,5-二羧酸-镉为三元混配合物;沙拉沙星-对苯二甲酸-锰配合物为三元混配合物,并且具有二维孔道网络结构。这些研究为研究药物的作用机理及开发新型药物提供了科学依据。
[Abstract]:Many pharmacological studies have shown that most biologically active drugs form complexes with metals that affect the clinical efficacy of drugs, and that there are many coordination sites in the structure of quinolones. In addition, the coordination polymers have potential applications in medicine and functional materials. Therefore, the synthesis and properties of metal complexes of quinolones have attracted much attention in recent years. Objective: to synthesize the metal complexes of enoxacin and salafloxacin and to characterize the crystal structure of the complexes, summarize the synthetic conditions and laws, analyze the topological types of crystals, and investigate the intermolecular forces. The geometric configuration of the complexes and the influence of the auxiliary ligands on the complexes were studied. It provides a reference for the synthesis of metal complexes of other quinolones, and provides a theoretical basis for further study of the effects of metal ions on the biological activities of these drugs. It provides scientific basis for developing new cheap quinolones and guiding clinical drugs. Methods: the coordination compounds were synthesized by hydrothermal method with enoxacin and salafloxacin as main ligands and transition metals as coordination reaction centers. The crystal structure of the complex was characterized by IR spectra. Results: four metal complexes of enoxacin and transition metal zinc (鈪,

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