Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids.
Antimicrob Agents Chemother
; 65(3)2021 02 17.
Article
em En
| MEDLINE
| ID: mdl-33361300
ABSTRACT
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 39.5 µM). 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.
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Base de dados:
MEDLINE
Assunto principal:
Trypanosoma cruzi
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Leishmania mexicana
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Doença de Chagas
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Antiprotozoários
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article