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

  • Bioorg Med Chem Lett. 2011 Aug 1;21(15):4498-502. doi: 10.1016/j.bmcl.2011.05.125.
Carlos Barea  1 ,  Adriana Pabón ,  Denis Castillo ,  Mirko Zimic ,  Miguel Quiliano ,  Silvia Galiano ,  Silvia Pérez-Silanes ,  Antonio Monge ,  Eric Deharo ,  Ignacio Aldana
Affiliations
  • 1. Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, Pamplona, Spain.
PMID: 21724395 DOI: 10.1016/j.bmcl.2011.05.125
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.