Barea, C. (Carlos)
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- New 1,4-di-N-oxide-quinoxaline-2-ylmethylene isonicotinic acid hydrazide derivatives as anti-Mycobacterieum tuberculosis agents(Elsevier, 2011) Aldana, I. (Ignacio); Ancizu, S. (Saioa); Torres, E. (Enrique); Pérez-Silanes, S. (Silvia); Monge, A. (Antonio); Moreno-de-Viguri, E. (Elsa); Barea, C. (Carlos)The increase in the prevalence of drug-resistant tuberculosis cases demonstrates the need of discovering new and promising compounds with antimycobacterial activity. As a continuation of our research and with the aim of identifying new antitubercular drugs candidates, a new series of quinoxaline 1,4-di-N-oxide derivatives containing isoniazid was synthesized and evaluated for in vitro anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv strain. Moreover, various drug-like properties of new compounds were predicted. Taking into account the biological results and the promising drug-likeness profile of these compounds, make them valid leads for further experimental research.
- New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities(Elsevier, 2011) Quiliano, M. (Miguel); Aldana, I. (Ignacio); Deharo, E. (Eric); Zimic, M. (Mirko); Pabon, A. (Adriana); Pérez-Silanes, S. (Silvia); Galiano, S. (Silvia); Monge, A. (Antonio); Barea, C. (Carlos); Castillo, D. (Denis)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
- New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities(Elsevier, 2011) Aldana, I. (Ignacio); Deharo, E. (Eric); Zimic, M. (Mirko); Pabon, A. (Adriana); Pérez-Silanes, S. (Silvia); Galiano, S. (Silvia); Monge, A. (Antonio); Barea, C. (Carlos); Castillo, D. (Denis)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
- Diseño, síntesis y evaluación biológica de nuevos derivados de 1,4-di-N-óxido de quinoxalina como agentes antimaláricos y leishmanicidas(Servicio de Publicaciones de la Universidad de Navarra, 2015) Barea, C. (Carlos); Aldana, I. (Ignacio)Malaria is by far the world¿s most important tropical parasitic disease and one of the oldest diseases known to mankind. Leishmaniasis is generally recognized for its cutaneous form which causes non-fatal disfiguring lesions, although epidemics of the potentially fatal visceral form cause thousands of deaths. The emergence of resistant parasites, the high cost and toxicity of current treatments call for the discovery of new drugs. The quinoxaline derivatives show very interesting biological properties and their interest in Medicinal Chemistry is still in progress. The oxidation of both nitrogens of this heterocyclic system in order to obtain quinoxaline 1,4-di-N-oxide derivatives increases the biological properties enormously. The experimental work presented in this memory is based on the fusion between quinoxaline 1,4-di-N-oxide derivatives and some active compounds against malaria and leishmania. This design is focused on the molecular hybridization as a strategy of combination of pharmacophoric moieties of different bioactive substances for producing a new hybrid compound with improved affinity and efficacy. As a result of different research projects, forty eight compounds have been designed, synthesized and evaluated in vitro against Plasmodium falciparum, Leishmania amazonensis and Leishmania infantum. The toxicity was also evaluated. Four compounds are highly active against Plasmodium falciparum, other four compounds are highly active against Leishmania amazonensis and seven against Leishmania infantum. Two compounds present better selectivity index than Amphotericin B.
- Antiplasmodial and leishmanicidal activities of 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives.(MDPI, 2012) Aldana, I. (Ignacio); Deharo, E. (Eric); Pabon, A. (Adriana); Deyssard, C. (Chloe); Pérez-Silanes, S. (Silvia); Galiano, S. (Silvia); Monge, A. (Antonio); Barea, C. (Carlos); Gonzalez, G. (Germán)Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Thirteen new 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives (CPCQs) were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against erythrocytic forms of Plasmodium falciparum and axenic forms of Leishmania infantum. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. None of the tested compounds was efficient against Plasmodium, but two of them showed good activity against Leishmania. Toxicity on VERO was correlated with leishmanicidal properties.
- New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities(MDPI, 2013) Aldana, I. (Ignacio); Deharo, E. (Eric); Pabon, A. (Adriana); Pérez-Silanes, S. (Silvia); Galiano, S. (Silvia); Monge, A. (Antonio); Barea, C. (Carlos); Gonzalez, G. (Germán)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.