New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities

Carlos Barea, Adriana Pabón, Denis Castillo, Mirko Zimic, Miguel Quiliano, Silvia Galiano, Silvia Pérez-Silanes, Antonio Monge, Eric Deharo, Ignacio Aldana

Research output: Contribution to journalArticle

Abstract

Continuing with our efforts to identify new active compounds against malaria and leishmaniasis, 14 new 3-amino-1,4-di-N-oxide quinoxaline-2- carbonitrile derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum Colombian FCR-3 strain and Leishmania amazonensis strain MHOM/BR/76/LTB-012A. Further computational studies were carried out in order to analyze graphic SAR and ADME properties. The results obtained indicate that compounds with one halogenous group substituted in position 6 and 7 provide an efficient approach for further development of antimalarial and antileishmanial agents. In addition, interesting ADME properties were found.

Original languageEnglish (US)
Pages (from-to)4498-4502
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number15
DOIs
StatePublished - Aug 1 2011

Keywords

  • Leishmaniasis
  • Malaria
  • N-Oxides
  • Quinoxaline

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Barea, C., Pabón, A., Castillo, D., Zimic, M., Quiliano, M., Galiano, S., Pérez-Silanes, S., Monge, A., Deharo, E., & Aldana, I. (2011). New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities. Bioorganic and Medicinal Chemistry Letters, 21(15), 4498-4502. https://doi.org/10.1016/j.bmcl.2011.05.125