New transition metal complexes containing imidazole rings endowed with potential antiamoebic activity
| العنوان: | New transition metal complexes containing imidazole rings endowed with potential antiamoebic activity |
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| المؤلفون: | Abdul Roouf Bhat, Fareeda Athar, Amir Azam, Mohmmad Younus Wani, Abilio J.F.N. Sobral |
| المصدر: | MedChemComm. 7:982-989 |
| بيانات النشر: | Royal Society of Chemistry (RSC), 2016. |
| سنة النشر: | 2016 |
| مصطلحات موضوعية: | Pharmacology, Nitroimidazole, biology, 010405 organic chemistry, Stereochemistry, Ligand, Organic Chemistry, Rational design, Pharmaceutical Science, Active site, 010402 general chemistry, 01 natural sciences, Biochemistry, 0104 chemical sciences, chemistry.chemical_compound, chemistry, Docking (molecular), Drug Discovery, Octahedral molecular geometry, biology.protein, Molecular Medicine, Imidazole, Chelation |
| الوصف: | 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. |
| تدمد: | 2040-2511 2040-2503 |
| DOI: | 10.1039/c6md00013d |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::8c5997852dc106437d034fabe18361c0 https://doi.org/10.1039/c6md00013d |
| رقم الانضمام: | edsair.doi...........8c5997852dc106437d034fabe18361c0 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 20402511 20402503 |
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| DOI: | 10.1039/c6md00013d |