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New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities

Authors :
Carlos Barea
Ignacio Aldana
Antonio Monge
German Gonzalez
Silvia Galiano
Silvia Pérez-Silanes
Eric Deharo
Adriana Pabón
Universidad de Navarra [Pamplona] (UNAV)
Universidad de Antioquia = University of Antioquia [Medellín, Colombia]
Universidad del Atlántico (UA)
Pharmacochimie et Biologie pour le Développement (PHARMA-DEV)
Institut de Recherche pour le Développement (IRD)-Institut de Chimie de Toulouse (ICT)
Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3)
Université de Toulouse (UT)-Université de Toulouse (UT)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Institut National Polytechnique (Toulouse) (Toulouse INP)
Université de Toulouse (UT)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3)
Université de Toulouse (UT)
Source :
Molecules; Volume 18; Issue 4; Pages: 4718-4727, Dadun. Depósito Académico Digital de la Universidad de Navarra, instname, Molecules, Repositorio UdeA, Universidad de Antioquia, instacron:Universidad de Antioquia, Molecules, 2013, 18 (4), pp.4718-4727. ⟨10.3390/molecules18044718⟩, Molecules, Vol 18, Iss 4, Pp 4718-4727 (2013)
Publication Year :
2013
Publisher :
MDPI, 2013.

Abstract

International audience; Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Continuing with our efforts to identify new compounds active against malaria and leishmaniasis, twelve new 1,4-di-N-oxide quinoxaline derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum FCR-3 strain, Leishmania infantum and Leishmania amazonensis. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. The results obtained indicate that a cyclopentyl derivative had the best antiplasmodial activity (2.9 µM), while a cyclohexyl derivative (2.5 µM) showed the best activity against L. amazonensis, and a 3-chloropropyl derivative (0.7 µM) showed the best results against L. infantum. All these compounds also have a Cl substituent in the R7 position

Details

Language :
English
ISSN :
14203049
Database :
OpenAIRE
Journal :
Molecules; Volume 18; Issue 4; Pages: 4718-4727, Dadun. Depósito Académico Digital de la Universidad de Navarra, instname, Molecules, Repositorio UdeA, Universidad de Antioquia, instacron:Universidad de Antioquia, Molecules, 2013, 18 (4), pp.4718-4727. ⟨10.3390/molecules18044718⟩, Molecules, Vol 18, Iss 4, Pp 4718-4727 (2013)
Accession number :
edsair.doi.dedup.....02ced1f632da8f03cd8c80f2c57ad9ff
Full Text :
https://doi.org/10.3390/molecules18044718⟩