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); Galiano, S. (Silvia); Pérez-Silanes, S. (Silvia); Monge, A. (Antonio); Deharo, E. (Eric); Aldana, I. (Ignacio)

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

Authors:

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

Editorial note:

CC BY-NC-ND

Note:

The authors gratefully acknowledge the ‘‘Oficina de Cooperación de la Embajada de Bélgica” for funding a Master Scholarship to Denis Castillo. Carlos Barea is indebted to the University of Navarra (Spain) for PhD scholarship

Citation:

Bioorganic & Medicinal Chemistry Letters 21 (2011) 4498–4502

Abstract

Continuing with the 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 to analyze graphic SAR and ADME properties were undertaken. Results 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/10171/61120

DOI:

10.1016/j.bmcl.2011.05.125

Appears in Collections:

DA - Farmacia - Orgánica - Artículos de revista

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