Sathisha M P, Shetti Ullas N, Revankar V K, Pai K S R
Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad 580 003, Karnataka, India.
Eur J Med Chem. 2008 Nov;43(11):2338-46. doi: 10.1016/j.ejmech.2007.10.003. Epub 2007 Oct 7.
The synthesis, structure, physico-chemical investigation and biological studies of some metal complexes of thiocarbohydrazone ligands are described. The ligand is obtained by condensation of N,N'-thiocarbohydrazide with 3-acetylcoumarin. The metal complexes of Co(II), Ni(II) and Cu(II) with bis(3-acetylcoumarin)thiocarbohydrazone were synthesized and isolated as solid products and characterized by analytical means as well as by spectral techniques such as FT-IR, (1)H NMR and EPR and UV spectrometry. The ligand acts as bidentate, through NO or NN, neutral in coordinating the M(II) ions. The bonding sites are the azomethine nitrogen, lactone carbonyl oxygen and respective anion counterparts. The metal complexes exhibit either octahedral or distorted octahedral structures. The complexes are found to be soluble in dimethylformamide and dimethylsulphoxide. Molar conductance values in dimethylsulphoxide indicate the non-electrolytic nature of the complexes. The compounds tested in present study have shown promising cytotoxic activity when screened using the in vitro method and at the same time were shown to have good activity when tested using the Ehrlich Ascites Carcinoma model. Preliminary antimicrobial screening shows the promising results against both bacterial and fungal strains.
描述了一些硫代碳酰肼配体金属配合物的合成、结构、物理化学研究及生物学研究。该配体通过N,N'-硫代碳酰肼与3-乙酰香豆素缩合得到。合成并分离出了钴(II)、镍(II)和铜(II)与双(3-乙酰香豆素)硫代碳酰肼的金属配合物作为固体产物,并通过分析手段以及FT-IR、(1)H NMR、EPR和紫外光谱等光谱技术对其进行了表征。该配体通过NO或NN作为双齿配体,在配位M(II)离子时呈中性。键合位点是偶氮甲碱氮、内酯羰基氧和相应的阴离子对应物。金属配合物呈现八面体或扭曲八面体结构。发现这些配合物可溶于二甲基甲酰胺和二甲基亚砜。在二甲基亚砜中的摩尔电导率值表明配合物的非电解质性质。在本研究中测试的化合物在采用体外方法进行筛选时显示出有前景的细胞毒性活性,同时在使用艾氏腹水癌模型进行测试时也显示出良好的活性。初步抗菌筛选显示对细菌和真菌菌株均有有前景的结果。