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Title
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Tetrahydrophthalazinone inhibitor of phosphodiesterase with in vitro activity against intracellular trypanosomatids
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Author
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Abstract
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| 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. |
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Language
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English
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Source (journal)
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Antimicrobial agents and chemotherapy. - Washington, D.C., 1972, currens
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Publication
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Washington, D.C.
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American Society for Microbiology
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2021
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ISSN
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0066-4804
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DOI
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10.1128/AAC.00960-20
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Volume/pages
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65
:3
(2021)
, 13 p.
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Article Reference
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AAC.00960-20
e00960-20
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ISI
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000619864100016
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Pubmed ID
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33361300
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Medium
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E-only publicatie
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Full text (Publisher's DOI)
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Full text (open access)
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