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

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

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 Colomb...

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Bibliographic Details
Main Authors: 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)
Format: info:eu-repo/semantics/article
Language:eng
Published: Elsevier 2012
Subjects:
Quinoxaline
N-oxides
Malaria
Leishmaniasis
Online Access:https://hdl.handle.net/10171/23742
Description
Summary: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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