Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids

Detalhes bibliográficos
Autor(a) principal: Araújo, Julianna Siciliano de
Data de Publicação: 2021
Outros Autores: Peres, Raiza Brandão, Silva, Patrícia Bernardino da, Batista, Marcos Meuser, Sterk, Geert Jan, Maes, Louis, Caljon, Guy, Leurs, Rob, Koning, Harry P. de, Kalejaiye, Titilola D., Soeiro, Maria de Nazareth Correia
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/48928
Resumo: Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil.
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spelling Araújo, Julianna Siciliano dePeres, Raiza BrandãoSilva, Patrícia Bernardino daBatista, Marcos MeuserSterk, Geert JanMaes, LouisCaljon, GuyLeurs, RobKoning, Harry P. deKalejaiye, Titilola D.Soeiro, Maria de Nazareth Correia2021-09-03T12:59:29Z2021-09-03T12:59:29Z2021ARAÚJO, Juliana Siciliano de et al. Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids. Antimicrobial Agents and Chemotherapy., v. 65, n. 3, e00960-20, 5 p, Feb. 2021.1098-6596https://www.arca.fiocruz.br/handle/icict/4892810.1128/AAC.00960-20engAmerican Society for MicrobiologyTrypanosoma cruziInibidor de fosfodiesteraseAtividade in vitroL. amazonensisL. infantumT. cruzicAMPin vitro activityPhosphodiesterase inhibitorTetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatidsinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleFundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil.Division of Medicinal Chemistry, Faculty of Sciences, Amsterdam Institute for Molecules, Medicines and Systems (AIMMS), Vrije Universiteit Amsterdam. Amsterdam, The Netherlands.Laboratory for Microbiology, Parasitology and Hygiene (LMPH). University of Antwerp. Antwerp, Belgium.Laboratory for Microbiology, Parasitology and Hygiene (LMPH). University of Antwerp. Antwerp, Belgium.Division of Medicinal Chemistry, Faculty of Sciences, Amsterdam Institute for Molecules, Medicines and Systems (AIMMS), Vrije Universiteit Amsterdam. Amsterdam, The Netherlands.Institute of Infection, Immunity & Inflammation, College of Medical, Veterinary & Life Sciences. University of Glasgow. Glasgow, United Kingdom.Institute of Infection, Immunity & Inflammation, College of Medical, Veterinary & Life Sciences. University of Glasgow. Glasgow, United Kingdom.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil.The phosphodiesterase inhibitor tetrahydrophthalazinone NPD-008 was explored by phenotypic in vitro screening, target validation, and ultrastructural approaches against Trypanosoma cruzi. NPD-008 displayed activity against different forms and strains of T. cruzi (50% effective concentration [EC50], 6.6 to 39.5mM). NPD-008 increased cAMP levels of T. cruzi and its combination with benznidazole gave synergistic interaction. It was also moderately active against intracellular amastigotes of Leishmania amazonensis and Leishmania infantum, confirming a potential activity profile as an antitrypanosomatid drug candidate.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/48928/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALJulianaAraujo_MNSoeiro_etal_IOC_2021.pdfJulianaAraujo_MNSoeiro_etal_IOC_2021.pdfapplication/pdf658226https://www.arca.fiocruz.br/bitstream/icict/48928/2/JulianaAraujo_MNSoeiro_etal_IOC_2021.pdf6e33ec1c677bb52136f3728821db79f5MD52TEXTJulianaAraujo_MNSoeiro_etal_IOC_2021.pdf.txtJulianaAraujo_MNSoeiro_etal_IOC_2021.pdf.txtExtracted 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dc.title.pt_BR.fl_str_mv Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
title Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
spellingShingle Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
Araújo, Julianna Siciliano de
Trypanosoma cruzi
Inibidor de fosfodiesterase
Atividade in vitro
L. amazonensis
L. infantum
T. cruzi
cAMP
in vitro activity
Phosphodiesterase inhibitor
title_short Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
title_full Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
title_fullStr Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
title_full_unstemmed Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
title_sort Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
author Araújo, Julianna Siciliano de
author_facet Araújo, Julianna Siciliano de
Peres, Raiza Brandão
Silva, Patrícia Bernardino da
Batista, Marcos Meuser
Sterk, Geert Jan
Maes, Louis
Caljon, Guy
Leurs, Rob
Koning, Harry P. de
Kalejaiye, Titilola D.
Soeiro, Maria de Nazareth Correia
author_role author
author2 Peres, Raiza Brandão
Silva, Patrícia Bernardino da
Batista, Marcos Meuser
Sterk, Geert Jan
Maes, Louis
Caljon, Guy
Leurs, Rob
Koning, Harry P. de
Kalejaiye, Titilola D.
Soeiro, Maria de Nazareth Correia
author2_role author
author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Araújo, Julianna Siciliano de
Peres, Raiza Brandão
Silva, Patrícia Bernardino da
Batista, Marcos Meuser
Sterk, Geert Jan
Maes, Louis
Caljon, Guy
Leurs, Rob
Koning, Harry P. de
Kalejaiye, Titilola D.
Soeiro, Maria de Nazareth Correia
dc.subject.other.pt_BR.fl_str_mv Trypanosoma cruzi
Inibidor de fosfodiesterase
Atividade in vitro
topic Trypanosoma cruzi
Inibidor de fosfodiesterase
Atividade in vitro
L. amazonensis
L. infantum
T. cruzi
cAMP
in vitro activity
Phosphodiesterase inhibitor
dc.subject.en.pt_BR.fl_str_mv L. amazonensis
L. infantum
T. cruzi
cAMP
in vitro activity
Phosphodiesterase inhibitor
description Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil.
publishDate 2021
dc.date.accessioned.fl_str_mv 2021-09-03T12:59:29Z
dc.date.available.fl_str_mv 2021-09-03T12:59:29Z
dc.date.issued.fl_str_mv 2021
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 ARAÚJO, Juliana Siciliano de et al. Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids. Antimicrobial Agents and Chemotherapy., v. 65, n. 3, e00960-20, 5 p, Feb. 2021.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/48928
dc.identifier.issn.pt_BR.fl_str_mv 1098-6596
dc.identifier.doi.none.fl_str_mv 10.1128/AAC.00960-20
identifier_str_mv ARAÚJO, Juliana Siciliano de et al. Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids. Antimicrobial Agents and Chemotherapy., v. 65, n. 3, e00960-20, 5 p, Feb. 2021.
1098-6596
10.1128/AAC.00960-20
url https://www.arca.fiocruz.br/handle/icict/48928
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 American Society for Microbiology
publisher.none.fl_str_mv American Society for Microbiology
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
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https://www.arca.fiocruz.br/bitstream/icict/48928/2/JulianaAraujo_MNSoeiro_etal_IOC_2021.pdf
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