Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.

Detalhes bibliográficos
Autor(a) principal: Bahl, Deepa
Data de Publicação: 2010
Outros Autores: Athar, Fareeda, Soares, Milena Botelho Pereira, Sá, Matheus Santos de, Moreira, Diogo Rodrigo Magalhães, Srivastava, Rajendra Mohan, Leite, Ana Cristina Lima, Azam, Amir
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/9001
Resumo: Jamia Millia Islamia. Department of Chemistry. Jamia Nagar, New Delhi, India
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spelling Bahl, DeepaAthar, FareedaSoares, Milena Botelho PereiraSá, Matheus Santos deMoreira, Diogo Rodrigo MagalhãesSrivastava, Rajendra MohanLeite, Ana Cristina LimaAzam, Amir2014-11-28T14:03:02Z2014-11-28T14:03:02Z2010BAHL, 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, 2010.1464-3391https://www.arca.fiocruz.br/handle/icict/9001engElsevierStructure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleJamia Millia Islamia. Department of Chemistry. Jamia Nagar, New Delhi, IndiaJamia Millia Islamia. Centre for Interdisciplinary Research in Basic Sciences. New Delhi, IndiaFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, Brasil / Hospital São Rafael. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisas Gonçalo Moniz. Salvador, BA, BrasilFederal University of Pernambuco. Centre for Natural Sciences. Department of Fundamental Chemistry. Recife, PE, BrasilFederal University of Pernambuco. Centre for Natural Sciences. Department of Fundamental Chemistry. Recife, PE, BrasilFederal University of Pernambuco. Centre for Health Sciences. Department of Pharmaceutical Sciences. Recife, PE, BrasilJamia Millia Islamia. Department of Chemistry. Jamia Nagar, New Delhi, IndiaA 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.Antiparasitic drugsDNAEntamoeba histolyticaMetal complexesPlasmodium falciparumThiosemicarbazonesAmebicidas/químicaAntimaláricos/químicaComplexos de Coordenação/químicaMetais/químicaTiossemicarbazida/químicaAmebicidas/síntese químicaAmebicidas/toxicidadeAnimaisAntimaláricos/síntese químicaAntimaláricos/toxicidadeComplexos de Coordenação/síntese químicaEntamoeba histolytica/efeitos de drogasCamundongosPlasmodium falciparum/efeitos de drogasBaço/citologiaBaço/efeitos de drogasTiossemicarbazida/síntese químicainfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-81914https://www.arca.fiocruz.br/bitstream/icict/9001/1/license.txt7d48279ffeed55da8dfe2f8e81f3b81fMD51ORIGINALBahl D Structure....pdfBahl D Structure....pdfapplication/pdf358432https://www.arca.fiocruz.br/bitstream/icict/9001/2/Bahl%20D%20Structure....pdffe33a421813c9a5e1a10977ada538369MD52TEXTBahl D Structure....pdf.txtBahl D Structure....pdf.txtExtracted texttext/plain48492https://www.arca.fiocruz.br/bitstream/icict/9001/3/Bahl%20D%20Structure....pdf.txt7652b9c5abd70ce59b7fb112b6a366b7MD53icict/90012023-03-15 14:33:03.328oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352023-03-15T17:33:03Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.
title Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.
spellingShingle Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.
Bahl, Deepa
Antiparasitic drugs
DNA
Entamoeba histolytica
Metal complexes
Plasmodium falciparum
Thiosemicarbazones
Amebicidas/química
Antimaláricos/química
Complexos de Coordenação/química
Metais/química
Tiossemicarbazida/química
Amebicidas/síntese química
Amebicidas/toxicidade
Animais
Antimaláricos/síntese química
Antimaláricos/toxicidade
Complexos de Coordenação/síntese química
Entamoeba histolytica/efeitos de drogas
Camundongos
Plasmodium falciparum/efeitos de drogas
Baço/citologia
Baço/efeitos de drogas
Tiossemicarbazida/síntese química
title_short Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.
title_full Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.
title_fullStr Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.
title_full_unstemmed Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.
title_sort Structure-activity relationships of mononuclear metal-thiosemicarbazone complexes endowed with potent antiplasmodial and antiamoebic activities.
author Bahl, Deepa
author_facet Bahl, Deepa
Athar, Fareeda
Soares, Milena Botelho Pereira
Sá, Matheus Santos de
Moreira, Diogo Rodrigo Magalhães
Srivastava, Rajendra Mohan
Leite, Ana Cristina Lima
Azam, Amir
author_role author
author2 Athar, Fareeda
Soares, Milena Botelho Pereira
Sá, Matheus Santos de
Moreira, Diogo Rodrigo Magalhães
Srivastava, Rajendra Mohan
Leite, Ana Cristina Lima
Azam, Amir
author2_role author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Bahl, Deepa
Athar, Fareeda
Soares, Milena Botelho Pereira
Sá, Matheus Santos de
Moreira, Diogo Rodrigo Magalhães
Srivastava, Rajendra Mohan
Leite, Ana Cristina Lima
Azam, Amir
dc.subject.en.pt_BR.fl_str_mv Antiparasitic drugs
DNA
Entamoeba histolytica
Metal complexes
Plasmodium falciparum
Thiosemicarbazones
topic Antiparasitic drugs
DNA
Entamoeba histolytica
Metal complexes
Plasmodium falciparum
Thiosemicarbazones
Amebicidas/química
Antimaláricos/química
Complexos de Coordenação/química
Metais/química
Tiossemicarbazida/química
Amebicidas/síntese química
Amebicidas/toxicidade
Animais
Antimaláricos/síntese química
Antimaláricos/toxicidade
Complexos de Coordenação/síntese química
Entamoeba histolytica/efeitos de drogas
Camundongos
Plasmodium falciparum/efeitos de drogas
Baço/citologia
Baço/efeitos de drogas
Tiossemicarbazida/síntese química
dc.subject.decs.pt_BR.fl_str_mv Amebicidas/química
Antimaláricos/química
Complexos de Coordenação/química
Metais/química
Tiossemicarbazida/química
Amebicidas/síntese química
Amebicidas/toxicidade
Animais
Antimaláricos/síntese química
Antimaláricos/toxicidade
Complexos de Coordenação/síntese química
Entamoeba histolytica/efeitos de drogas
Camundongos
Plasmodium falciparum/efeitos de drogas
Baço/citologia
Baço/efeitos de drogas
Tiossemicarbazida/síntese química
description Jamia Millia Islamia. Department of Chemistry. Jamia Nagar, New Delhi, India
publishDate 2010
dc.date.issued.fl_str_mv 2010
dc.date.accessioned.fl_str_mv 2014-11-28T14:03:02Z
dc.date.available.fl_str_mv 2014-11-28T14:03:02Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.citation.fl_str_mv 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.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/9001
dc.identifier.issn.none.fl_str_mv 1464-3391
identifier_str_mv 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.
1464-3391
url https://www.arca.fiocruz.br/handle/icict/9001
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
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instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
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