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Autor | Bahl, Deepa | |
Autor | Athar, Fareeda | |
Autor | Soares, Milena Botelho Pereira | |
Autor | Sá, Matheus Santos de | |
Autor | Moreira, Diogo Rodrigo Magalhães | |
Autor | Srivastava, Rajendra Mohan | |
Autor | Leite, Ana Cristina Lima | |
Autor | Azam, Amir | |
Fecha de acceso | 2014-11-28T14:03:02Z | |
Fecha de disponibilización | 2014-11-28T14:03:02Z | |
Fecha de publicación | 2010 | |
Referencia | BAHL, D. et al. Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities. Bioorganic & Medicinal Chemistry, v. 18, n. 18, p. 6857-6864, 2010. | pt_BR |
ISSN | 1464-3391 | |
URI | https://www.arca.fiocruz.br/handle/icict/9001 | |
Idioma | eng | pt_BR |
Editor | Elsevier | pt_BR |
Derechos de autor | open access | pt_BR |
Título | Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities. | pt_BR |
Tipo del documento | Article | pt_BR |
Resumen en Inglés | A useful concept for the rational design of antiparasitic drug candidates is the complexation of bioactive ligands with transition metals. In view of this, an investigation was conducted into a new set of metal complexes as potential antiplasmodium and antiamoebic agents, in order to examine the importance of metallic atoms, as well as the kind of sphere of co-ordination, in these biological properties. Four functionalized furyl-thiosemicarbazones (NT1–4) treated with divalent metals (Cu, Co, Pt, and Pd) to form the mononuclear metallic complexes of formula [M(L)2Cl2] or [M(L)Cl2] were examined. The pharmacological characterization, including assays against Plasmodium falciparum and Entamoeba histolytica, cytotoxicity to mammalian cells, and interaction with pBR 322 plasmid DNA was performed. Structure–activity relationship data revealed that the metallic complexation plays an essential role in antiprotozoal activity, rather than the simple presence of the ligand or metal alone. Important steps towards identification of novel antiplasmodium (NT1Cu, IC50 of 4.6 lM) and antiamoebic (NT2Pd, IC50 of 0.6 lM) drug prototypes were achieved. Of particular relevance to this work, these prototypes were able to reduce the proliferation of these parasites at concentrations that are not cytotoxic to mammalian cells. | pt_BR |
Afiliación | Jamia Millia Islamia. Department of Chemistry. Jamia Nagar, New Delhi, India | pt_BR |
Afiliación | Jamia Millia Islamia. Centre for Interdisciplinary Research in Basic Sciences. New Delhi, India | pt_BR |
Afiliación | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Salvador, BA, Brasil | pt_BR |
Afiliación | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Afiliación | Federal University of Pernambuco. Centre for Natural Sciences. Department of Fundamental Chemistry. Recife, PE, Brasil | pt_BR |
Afiliación | Federal University of Pernambuco. Centre for Natural Sciences. Department of Fundamental Chemistry. Recife, PE, Brasil | pt_BR |
Afiliación | Federal University of Pernambuco. Centre for Health Sciences. Department of Pharmaceutical Sciences. Recife, PE, Brasil | pt_BR |
Afiliación | Jamia Millia Islamia. Department of Chemistry. Jamia Nagar, New Delhi, India | pt_BR |
Palavras clave en Inglês | Antiparasitic drugs | pt_BR |
Palavras clave en Inglês | DNA | pt_BR |
Palavras clave en Inglês | Entamoeba histolytica | pt_BR |
Palavras clave en Inglês | Metal complexes | pt_BR |
Palavras clave en Inglês | Plasmodium falciparum | pt_BR |
Palavras clave en Inglês | Thiosemicarbazones | pt_BR |
DeCS | Amebicidas/química | pt_BR |
DeCS | Antimaláricos/química | pt_BR |
DeCS | Complexos de Coordenação/química | pt_BR |
DeCS | Metais/química | pt_BR |
DeCS | Tiossemicarbazida/química | pt_BR |
DeCS | Amebicidas/síntese química | pt_BR |
DeCS | Amebicidas/toxicidade | pt_BR |
DeCS | Animais | pt_BR |
DeCS | Antimaláricos/síntese química | pt_BR |
DeCS | Antimaláricos/toxicidade | pt_BR |
DeCS | Complexos de Coordenação/síntese química | pt_BR |
DeCS | Entamoeba histolytica/efeitos de drogas | pt_BR |
DeCS | Camundongos | pt_BR |
DeCS | Plasmodium falciparum/efeitos de drogas | pt_BR |
DeCS | Baço/citologia | pt_BR |
DeCS | Baço/efeitos de drogas | pt_BR |
DeCS | Tiossemicarbazida/síntese química | pt_BR |