Synthesis, characterization and in vitro Antiamoebic Activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones and their Palladium (II) and Ruthenium (II) Complexes
| Autor: | Amir Azam, Shailendra Kumar Singh, Neelam Bharti, Fehmida Naqvi |
|---|---|
| Rok vydání: | 2004 |
| Předmět: |
Thiosemicarbazones
Denticity Stereochemistry Nitro compound chemistry.chemical_element Chemical synthesis Ruthenium Metal Inhibitory Concentration 50 chemistry.chemical_compound Parasitic Sensitivity Tests Drug Discovery Organometallic Compounds Animals Moiety Amebicides Semicarbazone Pharmacology chemistry.chemical_classification Molecular Structure Spectrum Analysis Entamoeba histolytica Organic Chemistry General Medicine chemistry visual_art visual_art.visual_art_medium Palladium |
| Zdroj: | European Journal of Medicinal Chemistry. 39:459-465 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2004.02.003 |
| Popis: | Synthesis of new Palladium(II) and Ruthenium(II) complexes of the type, [Pd(L)Cl(2)] and [Ru(eta(4)-C(8)H(12))(L)Cl(2)] [where, L = thiosemicarbazones derived from 5-nitrothiophene-2-carboxaldehyde and cycloalkylaminothiocarbonyl hydrazines] have been isolated by the reaction of [Pd(DMSO)(2)Cl(2)] and [Ru(eta(4)-C(8)H(12))(CH(3)CN)(2)Cl(2)] with 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones. The spectral data revealed that the thiosemicarbazones act as bidentate ligands, making use of thionic sulphur and the azomethine nitrogen atom for coordination to the central metal ion. Microdilution method was used for the assessment of antiamoebic activity of all the compounds against HK-9 strain of Entamoeba histolytica. Among all the thiosemicarbazones, 5-NT-4-BPTSCN (3) showed significant antiamoebic activity (IC(50) - 2.56 microM). Enhancement of antiamoebic activity resulted by introducing palladium and ruthenium metals in the thiosemicarbazone moiety. All the Pd(II) and Ru(II) complexes of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones were found more active then their respective ligands. The complexes 1a-4a, 1b and 3b showed antiamoebic activity. |
| Databáze: | OpenAIRE |
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