Details der Publikation - Phenoxyacetohydrazones against Trypanosoma cruzi

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..

Medienart:	E-Artikel

Erscheinungsjahr:	2021
Erschienen:	2021

Enthalten in:	Zur Gesamtaufnahme - volume:30
Enthalten in:	Medicinal chemistry research - 30(2021), 9 vom: 27. Juli, Seite 1703-1712

Sprache:	Englisch

Beteiligte Personen:	Capelini, Camila [VerfasserIn] de Souza, Kátia R. [VerfasserIn] Barbosa, Juliana M. C. [VerfasserIn] Salomão, Kelly [VerfasserIn] Sales Junior, Policarpo A. [VerfasserIn] Murta, Silvane M. F. [VerfasserIn] Wardell, Solange M. S. V. [VerfasserIn] Wardell, James L. [VerfasserIn] da Silva, Edson F. [VerfasserIn] Carvalho, Samir A. [VerfasserIn]

Links:	Volltext [lizenzpflichtig]

Anmerkungen:	© The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature 2021. corrected publication 2021

doi:	10.1007/s00044-021-02768-9

funding:
Förderinstitution / Projekttitel:

PPN (Katalog-ID):	OLC2127140370

Internformat


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Phenoxyacetohydrazones against Trypanosoma cruzi

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