Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids.
Antimicrob Agents Chemother
; 65(3)2021 02 17.
Article
en 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.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Trypanosoma cruzi
/
Leishmania mexicana
/
Enfermedad de Chagas
/
Antiprotozoarios
Límite:
Humans
Idioma:
En
Revista:
Antimicrob Agents Chemother
Año:
2021
Tipo del documento:
Article
País de afiliación:
Brasil