New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities
Palabras clave : 
Quinoxaline
N-oxides
Malaria
Leishmaniasis
Fecha incorporación: 
2011
Editorial : 
Elsevier
ISSN: 
0960-894X
Cita: 
Barea C, Pabon A, Castillo D, Zimic M, Quiliano M, Galiano S, et al. 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):4498-4502.
Resumen
Continuing with our efforts to identify new active compounds against malaria and leishmaniasis, fourteen 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

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Descripción: 
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