Author | Bahl, Deepa | |
Author | Athar, Fareeda | |
Author | Soares, Milena Botelho Pereira | |
Author | Sá, Matheus Santos de | |
Author | Moreira, Diogo Rodrigo Magalhães | |
Author | Srivastava, Rajendra Mohan | |
Author | Leite, Ana Cristina Lima | |
Author | Azam, Amir | |
Access date | 2014-11-28T14:03:02Z | |
Available date | 2014-11-28T14:03:02Z | |
Document date | 2010 | |
Citation | 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 | |
Language | eng | pt_BR |
Publisher | Elsevier | pt_BR |
Rights | open access | pt_BR |
Title | Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities. | pt_BR |
Type | Article | pt_BR |
Abstract | 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 |
Affilliation | Jamia Millia Islamia. Department of Chemistry. Jamia Nagar, New Delhi, India | pt_BR |
Affilliation | Jamia Millia Islamia. Centre for Interdisciplinary Research in Basic Sciences. New Delhi, India | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Salvador, BA, Brasil | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
Affilliation | Federal University of Pernambuco. Centre for Natural Sciences. Department of Fundamental Chemistry. Recife, PE, Brasil | pt_BR |
Affilliation | Federal University of Pernambuco. Centre for Natural Sciences. Department of Fundamental Chemistry. Recife, PE, Brasil | pt_BR |
Affilliation | Federal University of Pernambuco. Centre for Health Sciences. Department of Pharmaceutical Sciences. Recife, PE, Brasil | pt_BR |
Affilliation | Jamia Millia Islamia. Department of Chemistry. Jamia Nagar, New Delhi, India | pt_BR |
Subject | Antiparasitic drugs | pt_BR |
Subject | DNA | pt_BR |
Subject | Entamoeba histolytica | pt_BR |
Subject | Metal complexes | pt_BR |
Subject | Plasmodium falciparum | pt_BR |
Subject | 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 |