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

Barea, C. (Carlos); Pabon, A. (Adriana); Castillo, D. (Denis); Zimic, M. (Mirko); Quiliano, M. (Miguel); Galiano, S. (Silvia); Pérez-Silanes, S. (Silvia); Monge, A. (Antonio); Deharo, E. (Eric); Aldana, I. (Ignacio)

Keywords:

Quinoxaline
N-oxides
Malaria
Leishmaniasis

Issue Date:

2011

Publisher:

Elsevier

ISSN:

0960-894X

Citation:

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.

Abstract

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

URI:

https://hdl.handle.net/10171/23742

DOI:

http://dx.doi.org/10.1016/j.bmcl.2011.05.125

Appears in Collections:

DA - CIFA - I+D de medicamentos - Artículos de revistas
DA - Farmacia - Orgánica - Artículos de revista

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