New Amide Derivatives of Quinoxaline 1,4-di-N-Oxide with Leishmanicidal and Antiplasmodial Activities.

Barea, Carlos; Pabón, Adriana; Pérez-Silanes, Silvia; Galiano, Silvia; Gonzalez, German; Monge, Antonio; Deharo, Eric; Aldana, Ignacio

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 μM), while a cyclohexyl derivative (2.5 μM) showed the best activity against L. amazonensis, and a 3-chloropropyl derivative (0.7 μM) showed the best results against L. infantum. All these compounds also have a Cl substituent in the R7 position.

MALARIA; LEISHMANIASIS; AMIDE derivatives; QUINOXALINES; PARASITIC diseases; PLASMODIUM falciparum

Molecules, 2013, Vol 18, Issue 4, p4718

1420-3049

Academic Journal

10.3390/molecules18044718