A Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity Against Intracellular Trypanosomatids.

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 (EC50 = 6.6 - 39.5 μM), increased cAMP levels of T. cruzi and its combination with Bz gave synergistic interaction. It was also moderately active against intracellular amastigotes of Leishmania amazonensisandL. infantum, confirming a potential activity profile as an antitrypanosomatid drug candidate.

authors

de Araújo JS,Peres RB,Bernardino da Silva P,Batista MM,Sterk GJ,Maes L,Caljon G,Leurs R,de Koning HP,Kalejaiye TD,Soeiro MNC

doi

10.1128/AAC.00960-20

subject

Has Abstract

pub_date

2020-12-23 00:00:00

eissn

0066-4804

issn

1098-6596

pii

AAC.00960-20

pub_type

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