Phenoxyacetohydrazones against Trypanosoma cruzi
Abstract Herein, we reported the design, synthesis, antitrypanosomal and cytotoxic evaluation of a new phenoxyacetohydrazones series. All derivatives were assayed against bloodstream trypomastigote forms of T. cruzi (Y strain) and intracellular amastigotes using the model of L-929 cells infected with trypomastigotes of the Tulahuen strain. Compound (E)-N′-(3.4-dihydroxybenzylidene)-2-phenoxyacetohydrazide (11) showed activity against trypomastigotes ($ IC_{50} $/24 h = 10.3 µM) equivalent to that of benznidazole and with selectivity index (SI) = 46. Against infected cultures, (E)-N′-((5-nitrofuran-2-yl) methylene)-2-phenoxyacetohydrazide (19) was active at the nanomolar range ($ IC_{50} $/96 h = 40 nM), being about 38-fold more active than the standard drug and with SI equal to 2500. Thus, derivatives 11 and 19 could be considered a good prototypes for the development of new candidates for Chagas disease therapy..
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E-Artikel |
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Erscheinungsjahr: |
2021 |
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Erschienen: |
2021 |
Enthalten in: |
Zur Gesamtaufnahme - volume:30 |
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Enthalten in: |
Medicinal chemistry research - 30(2021), 9 vom: 27. Juli, Seite 1703-1712 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Capelini, Camila [VerfasserIn] |
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Links: |
Volltext [lizenzpflichtig] |
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BKL: |
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Anmerkungen: |
© The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature 2021. corrected publication 2021 |
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doi: |
10.1007/s00044-021-02768-9 |
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funding: |
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PPN (Katalog-ID): |
SPR044789947 |
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