Juneja Annu, Macedo Tais Soares, Magalhaes Moreira Diogo Rodrigo, Pereira Soares Milena Botelho, Lima Leite Ana Cristina, Kelle de Andrade Lemoine Neves Juliana, Alves Pereira Valeria Rego, Avecilla Fernando, Azam Amir
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Centro de Pesquisas Gonçalo Moniz, Fundação Oswaldo Cruz, Rua Waldemar Falcão, 121, Candeal, 40296-710 Salvador, BA, Brazil.
Eur J Med Chem. 2014 Mar 21;75:203-10. doi: 10.1016/j.ejmech.2014.01.051. Epub 2014 Jan 31.
A terpyridine ligand Fctpy was reacted with divalent metals (Cu, Co, Mn, Ni and Zn), yielding five complexes of general formula [Metal(Fctpy)2][PF6]2. The structure of Fctpy was determined by single crystal X-ray diffraction studies. The complexes characterized using various spectroscopic techniques suggested an octahedral geometry around the central metal ion. These complexes were screened for their antiamoebic, trypanocidal and antimalarial activities. It was found that, complexes 2 and 3 showed better IC50 values than metronidazole against HM1:IMSS strain of Entamoeba histolytica. A substantial parasitic inhibition was not observed for the trypanocidal activity. However, for the erythrocytic stage of W2 strain of Plasmodium falciparum, the complexes inhibited β-hematin formation. At the concentration of 10 μg/mL, these complexes did not display toxicity.
一种三联吡啶配体Fctpy与二价金属(铜、钴、锰、镍和锌)反应,生成了通式为[金属(Fctpy)₂][PF₆]₂的五种配合物。Fctpy的结构通过单晶X射线衍射研究确定。使用各种光谱技术对这些配合物进行表征,结果表明中心金属离子周围呈八面体几何构型。对这些配合物的抗阿米巴、抗锥虫和抗疟活性进行了筛选。结果发现,配合物2和3对溶组织内阿米巴HM1:IMSS菌株的IC₅₀值比甲硝唑更好。对于抗锥虫活性,未观察到显著的寄生虫抑制作用。然而,对于恶性疟原虫W2菌株的红细胞阶段,这些配合物抑制了β-血红素的形成。在10μg/mL的浓度下,这些配合物未显示出毒性。