Barea C., Pabon A., Perez-Silanes S., Galiano S., Gonzalez G., Monge A., Deharo Eric, Aldana I. (2013). New amide derivatives of quinoxaline 1,4-di-N-Oxide with leishmanicidal and antiplasmodial activities. Molecules, 18 (4), p. 4718-4727. ISSN 1420-3049.
Titre du document
New amide derivatives of quinoxaline 1,4-di-N-Oxide with leishmanicidal and antiplasmodial activities
Barea C., Pabon A., Perez-Silanes S., Galiano S., Gonzalez G., Monge A., Deharo Eric, Aldana I.
Source
Molecules, 2013,
18 (4), p. 4718-4727 ISSN 1420-3049
Malaria and leishmaniasis are two of the World's most important tropical parasitic diseases. Continuing with our efforts to identify new compounds active against malaria and leishmaniasis, twelve new 1,4-di-N-oxide quinoxaline derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum FCR-3 strain, Leishmania infantum and Leishmania amazonensis. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. The results obtained indicate that a cyclopentyl derivative had the best antiplasmodial activity (2.9 mu M), while a cyclohexyl derivative (2.5 mu M) showed the best activity against L. amazonensis, and a 3-chloropropyl derivative (0.7 mu M) showed the best results against L. infantum. All these compounds also have a Cl substituent in the R-7 position.
