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合成并评价钯(II)水杨醛亚胺缩硫代氨基脲配合物对阴道毛滴虫的体外活性。

Synthesis and in vitro evaluation of palladium(II) salicylaldiminato thiosemicarbazone complexes against Trichomonas vaginalis.

机构信息

Department of Chemistry, University of Cape Town, Rondebosch, South Africa.

出版信息

J Inorg Biochem. 2011 Dec;105(12):1562-8. doi: 10.1016/j.jinorgbio.2011.07.023. Epub 2011 Aug 6.

DOI:10.1016/j.jinorgbio.2011.07.023
PMID:22071079
Abstract

Eight mononuclear Pd(II) complexes containing salicylaldiminato thiosemicarbazones (saltsc-R; where R=H (1), 3-OMe (2), 3-(t)Bu (3) and 5-Cl (4)) as dinegative tridentate ligands were prepared by the reaction of the corresponding thiosemicarbazone with the precursor Pd(L)(2)Cl(2) (L=phosphatriazaadamantane or 4-picoline) in the presence of a weak base. These complexes (9-16) were characterised by a range of spectroscopic and analytical techniques including NMR spectroscopy and X-ray diffraction. These complexes along with four other Pd(II) analogues (5-8) were screened for activity in vitro against the Trichomonas vaginalis parasite. Preliminary results show that the type of ancillary ligand as well as the substituents on the aromatic ring of the salicylaldiminato thiosemicarbazone ligand influences the antiparasitic activity of these complexes.

摘要

八个单核钯(II)配合物,含有水杨醛亚胺硫代缩氨基脲(盐 sc-R;其中 R=H(1),3-OMe(2),3-(t)Bu(3)和 5-Cl(4))作为二价三齿配体,是通过相应的硫代缩氨基脲与前体 Pd(L)(2)Cl(2)(L=磷杂氮金刚烷或 4-吡啶)在弱碱存在下反应制备的。这些配合物(9-16)通过一系列光谱和分析技术进行了表征,包括 NMR 光谱和 X 射线衍射。这些配合物以及另外四个钯(II)类似物(5-8)在体外针对阴道毛滴虫寄生虫进行了活性筛选。初步结果表明,辅助配体的类型以及水杨醛亚胺硫代缩氨基脲配体芳环上的取代基影响这些配合物的抗寄生虫活性。

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