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Issue 5, 2016
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New transition metal complexes containing imidazole rings endowed with potential antiamoebic activity

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Abstract

A useful concept for the rational design of anti-protozoal drug candidates is the complexation of bioactive ligands with transition metals. We previously reported that nitroimidazole acylhydrazones possess excellent antiamoebic activity; in this study, we synthesized some CuII, CoII and NiII metal complexes and chose 2-(5-methyl-2-nitro-1H-imidazol-1-yl)-N′-[(E)-pyridin-2-ylmethylidene]acetohydrazide as a ligand. Physical and spectroscopic characterization revealed a distorted octahedral geometry for the complexes. The pharmacological characterization, including assays against Entamoeba histolytica and cytotoxicity to mammalian cells, revealed that chelation improves the antiamoebic activity of the ligand. Docking of the ligand with thioredoxin reductase (EhTrR), a promising target for the treatment of amoebiasis, showed that the inhibitor snugly fits the active site of the target enzyme, which may well explain the excellent inhibitory activity.

Graphical abstract: New transition metal complexes containing imidazole rings endowed with potential antiamoebic activity

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Supplementary files

Article information


Submitted
11 Jan 2016
Accepted
03 Mar 2016
First published
04 Mar 2016

Med. Chem. Commun., 2016,7, 982-989
Article type
Research Article

New transition metal complexes containing imidazole rings endowed with potential antiamoebic activity

M. Y. Wani, A. R. Bhat, A. Azam, F. Athar and A. J. F. N. Sobral, Med. Chem. Commun., 2016, 7, 982
DOI: 10.1039/C6MD00013D

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