Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Outros Autores: | , , , , , , , , , |
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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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 |
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eng |
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eng |
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info:eu-repo/semantics/openAccess |
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openAccess |
dc.publisher.none.fl_str_mv |
American Society for Microbiology |
publisher.none.fl_str_mv |
American Society for Microbiology |
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Repositório Institucional da FIOCRUZ (ARCA) |
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