Department of Chemistry, University of Fort Hare, Alice 5700, South Africa.
Bioinorg Chem Appl. 2013;2013:549549. doi: 10.1155/2013/549549. Epub 2013 Mar 12.
Pd(II) and Pt(II) complexes of trimethoprim and pyrimethamine were synthesized and characterized by elemental analysis, UV-Vis, FTIR, and NMR spectroscopy. The complexes are formulated as four coordinate square planar species containing two molecules of the drugs and two chloride or thiocyanate ions. The coordination of the metal ions to the pyrimidine nitrogen atom of the drugs was confirmed by spectroscopic analyses. The complexes were screened for their antibacterial activities against eight bacterial isolates. They showed varied activities with the active metal complexes showing more enhanced inhibition than either trimethoprim or pyrimethamine. The Pd(II) complexes of pyrimethamine showed unique inhibitory activities against P. aeruginosa and B. pumilus, and none of the other complexes or the drugs showed any activity against these bacteria isolates. The MIC and MBC determinations revealed that these Pd(II) complexes are the most active. Structure activity relationship showed that Pt(II) complexes containing chloride ions are more active, while for Pd(II) complexes containing thiocyanate ions showed more enhanced activity than those containing chloride ions.
二价钯(Pd(II))和二价铂(Pt(II))与三甲氧苄氨嘧啶和乙胺嘧啶的配合物通过元素分析、紫外-可见光谱、傅里叶变换红外光谱和核磁共振光谱进行了合成和表征。这些配合物的分子式为含有两种药物分子和两种氯离子或硫氰酸根离子的四配位平面正方形物种。金属离子与药物中嘧啶氮原子的配位通过光谱分析得到了证实。这些配合物对 8 种细菌分离株的抗菌活性进行了筛选。它们表现出不同的活性,活性金属配合物的抑制作用比三甲氧苄氨嘧啶或乙胺嘧啶更强。乙胺嘧啶的 Pd(II)配合物对铜绿假单胞菌和短小芽孢杆菌具有独特的抑制活性,而其他配合物或药物对这些细菌分离株均无活性。MIC 和 MBC 测定表明这些 Pd(II)配合物最具活性。构效关系表明,含氯离子的 Pt(II)配合物更具活性,而含硫氰酸根离子的 Pd(II)配合物比含氯离子的配合物具有更高的活性。