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TETRAHYDROPHTHALAZINONE INHIBITOR OF PHOSPHODIESTERASE WITH IN VITRO ACTIVITY AGAINST INTRACELLULAR TRYPANOSOMATIDS
L. infantum
T. cruzi
cAMP
in vitro activity
Phosphodiesterase inhibitor
Autor
Afiliación
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.
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.
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.
Resumen en ingles
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.
Palabras clave en ingles
L. amazonensisL. infantum
T. cruzi
cAMP
in vitro activity
Phosphodiesterase inhibitor
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