Back to Search Start Over

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

Authors :
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)
Source :
Dadun: Depósito Académico Digital de la Universidad de Navarra, Universidad de Navarra, Dadun. Depósito Académico Digital de la Universidad de Navarra, Consejo Superior de Investigaciones Científicas (CSIC)
Publication Year :
2011
Publisher :
Elsevier, 2011.

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

Details

Database :
OpenAIRE
Journal :
Dadun: Depósito Académico Digital de la Universidad de Navarra, Universidad de Navarra, Dadun. Depósito Académico Digital de la Universidad de Navarra, Consejo Superior de Investigaciones Científicas (CSIC)
Accession number :
edsair.dedup.wf.001..9b4493fec9ee87448e0d615cd6fd658b