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钯和铂与氟喹诺酮配合物的合成及其抗结核活性

Synthesis and antitubercular activity of palladium and platinum complexes with fluoroquinolones.

作者信息

Vieira Lígia Maria M, de Almeida Mauro V, Lourenço Maria Cristina S, Bezerra Flávio Augusto F M, Fontes Ana Paula S

机构信息

Departamento de Química, Universidade Federal de Juiz de Fora, 36036-900 Juiz de Fora, MG, Brazil.

出版信息

Eur J Med Chem. 2009 Oct;44(10):4107-11. doi: 10.1016/j.ejmech.2009.05.001. Epub 2009 May 15.

Abstract

The fluoroquinolones are an important family of synthetic antimicrobial agents being clinically used over the past thirty years. In addition, some fluoroquinolones have been used in the development of anticancer drugs, and others have demonstrated anti-HIV activity. Furthermore, there has been some additional work investigating the effect of metal ions on biological activity. Aiming to obtain novel palladium(II) and platinum(II) complexes that exhibit biological activity, we have synthesized complexes using fluoroquinolones (ciprofloxacin, levofloxacin, ofloxacin, sparfloxacin, and gatifloxacin) as ligands. The compounds were characterized using IR and NMR spectroscopy, thermogravimetric and elemental analyses. The complexes show activity against Mycobacterium tuberculosis strain H(37)Rv. The minimal inhibitory concentration (MIC) of the complexes was determined.

摘要

氟喹诺酮类是一类重要的合成抗菌剂,在过去三十年中一直用于临床。此外,一些氟喹诺酮类已被用于抗癌药物的研发,还有一些表现出抗HIV活性。此外,还有一些额外的工作在研究金属离子对生物活性的影响。为了获得具有生物活性的新型钯(II)和铂(II)配合物,我们使用氟喹诺酮类(环丙沙星、左氧氟沙星、氧氟沙星、司帕沙星和加替沙星)作为配体合成了配合物。通过红外光谱、核磁共振光谱、热重分析和元素分析对这些化合物进行了表征。这些配合物对结核分枝杆菌H(37)Rv菌株显示出活性。测定了配合物的最低抑菌浓度(MIC)。

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