Antiprotozoal activity of (e)-cinnamic N-acylhydrazone derivatives
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 2803550
Author(s) Carvalho, Samir Aquino; Kaiser, Marcel; Brun, Reto; da Silva, Edson Ferreira; Fraga, Carlos Alberto Manssour
Author(s) at UniBasel Kaiser, Marcel
Brun, Reto
Year 2014
Title Antiprotozoal activity of (e)-cinnamic N-acylhydrazone derivatives
Journal Molecules
Volume 19
Number 12
Pages / Article-Number 20374-81
Keywords antiprotozoal activity, Leishmania, Trypanosoma, N-acylhydrazone, (E)-cinnamic acid derivatives, molecular hybridization
Abstract

A series of 14 (E)-cinnamic N-acylhydrazone derivatives, designed through molecular hybridization between the (E)-1-(benzo[d][1,3]dioxol-5-yl)-3-(4-bromophenyl)prop-2-en-1-one and (E)-3-hydroxy-N'-((2-hydroxynaphthalen-1-yl)methylene)-7-methoxy-2-naphthohydrazide, were tested for in vitro antiparasitic activity upon axenic amastigote forms of Leishmania donovani and bloodstream forms of Trypamosoma brucei rhodesiense. The derivative (2E)-3-(4-hydroxy-3-methoxy-5-nitrophenyl)-N'-[(1E)-phenylmethylene]acrylohydrazide showed moderate antileishmanial activity (IC50 = 6.27 µM) when compared to miltefosine, the reference drug (IC50 = 0.348 µM). However, the elected compound showed an excellent selectivity index; in one case it was not cytotoxic against mammalian L-6 cells. The most active antitrypanosomal compound, the derivative (E)-N'-(3,4-dihydroxybenzylidene)cinnamohydrazide (IC50 = 1.93 µM), was cytotoxic against mammalian L-6 cells.

Publisher MDPI
ISSN/ISBN 1420-3049
edoc-URL http://edoc.unibas.ch/dok/A6329146
Full Text on edoc No
Digital Object Identifier DOI 10.3390/molecules191220374
PubMed ID http://www.ncbi.nlm.nih.gov/pubmed/25490429
ISI-Number WOS:000346793200063
Document type (ISI) Journal Article
 
   

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