Novel bidentate complexes of Cu(II) derived from 5-nitrofuran-2-carboxaldehyde thiosemicarbazones with antiamoebic activity against E. histolytica
| Autor: | Fehmida Naqvi, Amir Azam, Sangita Sharma, Mannar R. Maurya, Fareeda Athar |
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| Rok vydání: | 2005 |
| Předmět: |
Thiosemicarbazones
Magnetic Resonance Spectroscopy Denticity Spectrophotometry Infrared Nitrofurans Stereochemistry medicine.drug_class Antiprotozoal Agents Nitro compound Chemical synthesis Inhibitory Concentration 50 Entamoeba histolytica chemistry.chemical_compound Drug Discovery Octahedral molecular geometry Organometallic Compounds medicine Animals Humans Semicarbazone Nitrofuran Pharmacology chemistry.chemical_classification Molecular Structure biology Organic Chemistry General Medicine Nuclear magnetic resonance spectroscopy biology.organism_classification chemistry Copper |
| Zdroj: | European Journal of Medicinal Chemistry. 40:557-562 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2005.01.003 |
| Popis: | The novel analogues of 5-nitrofuran-2-carboxaldehyde thiosemicarbazones 1-10 were synthesized and their copper(II) complexes 1a-10a were obtained by means of coordination with cupric chloride. All these compounds have been characterized by elemental analysis, IR, electronic spectra and thermogravimetric patterns while ligands have also been characterized by 1H NMR spectral studies. These copper complexes are bidentate and possess octahedral geometry around Cu(II) ion. Their antiamoebic activities were carried out to ascertain their effectiveness in comparison to their corresponding thiosemicarbazones. A number of these complexes possess noteworthy potencies towards HK-9 strain of Entamoeba histolytica in vitro. The complexes 2a-7a, 9a and 10a showed less IC50 value than metronidazole, the drug of choice for amoebiasis. Moreover, complexes 2a and 9a have shown the most promising antiamoebic activities (IC50 = 0.38 microM of 2a and IC50 = 0.34 microM of 9a versus IC50 = 1.81 microM of metronidazole). These results indicate that the metallated thiosemicarbazone may be lead molecule to inhibit growth of E. histolytica. |
| Databáze: | OpenAIRE |
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