New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities

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 antima...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2013-04, Vol.18 (4), p.4718-4727
Main Authors: Barea, Carlos, Pabón, Adriana, Pérez-Silanes, Silvia, Galiano, Silvia, Gonzalez, German, Monge, Antonio, Deharo, Eric, Aldana, Ignacio
Format: Article
Language:English
Subjects:
1,4-di-N-oxide
Amides - chemistry
Animals
Antimalarials - chemistry
Antimalarials - pharmacology
Antimalarials - toxicity
Antiparasitic Agents - chemistry
Antiparasitic Agents - pharmacology
Antiparasitic Agents - toxicity
antiplasmodial
Cercopithecus aethiops
Humans
Inhibitory Concentration 50
Leishmania - drug effects
Leishmania infantum - drug effects
leishmanicidal
Life Sciences
Malaria
Oxides - chemistry
Parasitic diseases
Parasitic Sensitivity Tests
Plasmodium - drug effects
Plasmodium falciparum - drug effects
quinoxaline
Quinoxalines - chemistry
Quinoxalines - pharmacology
Quinoxalines - toxicity
Structure-Activity Relationship
Toxicity
Tropical diseases
Vero Cells
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Summary: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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules18044718