【摘要】：許多藥理學(xué)的研究表明：大部分具有生物活性的藥物與金屬形成配合物后影響藥物的臨床療效；再者,喹諾酮類藥物的結(jié)構(gòu)上存在多個配位點,為構(gòu)筑配合物體系提供了可能性；另外,其配位聚合物在醫(yī)藥及功能材料中具有潛在的應(yīng)用前景。因此,喹諾酮類藥物金屬配合物的合成及性質(zhì)研究在近幾年來受到了極大的關(guān)注。目的：通過合成依諾沙星及沙拉沙星藥物金屬配合物和表征配合物的晶體結(jié)構(gòu),總結(jié)合成條件及規(guī)律,分析晶體的拓撲類型,考察分子間的作用力,研究配合物的幾何構(gòu)型及輔助配體對配合物的影響,探討藥物與金屬的配位方式。為其它喹諾酮類藥物金屬配合物的合成提供參考,為進一步研究金屬離子對此類藥物生物活性的影響奠定理論基礎(chǔ),為開發(fā)新型價格低廉的喹諾酮類藥物及指導(dǎo)臨床用藥提供科學(xué)依據(jù)。方法：以依諾沙星和沙拉沙星藥物為主要配體,以過渡金屬為配位反應(yīng)中心,采用水熱法合成配位化合物；利用X-射線單晶衍射技術(shù),元素分析、紅外光譜表征了配合物的晶體結(jié)構(gòu)。結(jié)果：合成出符合晶體學(xué)要求的4種金屬配合物,分別是依諾沙星與過渡金屬鋅(Ⅱ)、銅(Ⅱ)構(gòu)筑的兩個配合物；依諾沙星、噻吩-2,5-二羧酸與過渡金屬鎘構(gòu)筑的配合物；沙拉沙星、對苯二甲酸與過渡金屬錳(Ⅱ)構(gòu)筑的配合物。結(jié)論：本論文闡述了4個由喹諾酮類藥物與金屬所構(gòu)筑配合物的晶體結(jié)構(gòu)。其中,依諾沙星-鋅(Ⅱ)、銅(Ⅱ)配合物為離子型化合物；依諾沙星-噻吩-2,5-二羧酸-鎘為三元混配合物；沙拉沙星-對苯二甲酸-錳配合物為三元混配合物,并且具有二維孔道網(wǎng)絡(luò)結(jié)構(gòu)。這些研究為研究藥物的作用機理及開發(fā)新型藥物提供了科學(xué)依據(jù)。
[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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