Tetrahydrophthalazinone inhibitor of phosphodiesterase with in vitro activity against intracellular trypanosomatids

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 (EC 50 = 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 amazonensis and L. infantum , confirming a potential activity profile as an antitrypanosomatid drug candidate.

Publication year:2021

Keywords:A1 Journal article

BOF-keylabel:yes

BOF-publication weight:3

CSS-citation score:1

Authors:International

Authors from:Higher Education

Accessibility:Open