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Molecules 2009, 14(6), 2256-2272; doi:10.3390/molecules14062256

Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-N-oxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs

1
Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, C/Irunlarrea s/n, 31008 Pamplona, Spain
2
Laboratorio de Química Orgánica, Facultad de Ciencias/Facultad de Química, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay
*
Authors to whom correspondence should be addressed.
Received: 2 June 2009 / Revised: 15 June 2009 / Accepted: 17 June 2009 / Published: 22 June 2009
(This article belongs to the Special Issue Neglected Diseases: Medicinal Chemistry and Natural Product Chemistry)
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Abstract

Neglected diseases represent a major health problem. It is estimated that one third of the world population is infected with tuberculosis (TB). Besides TB, Chagas disease, affects approximately 20 million people. Quinoxalines display great activities against TB and Chagas. Forty new quinoxaline 1,4-di-N-oxide derivatives have been prepared and tested against M. tuberculosis and T. cruzi. Carboxylic acid quinoxaline 1,4-di-N-oxides (CAQDOs) 5 and 17 showed MIC values on the same order as the reference antituberculosis drug, rifampicin. Meanwhile, CAQDOs 12 and 22 presented IC50 values in the same order as the anti-chagasic drug, nifurtimox.
Keywords: quinoxaline; neglected diseases; Mycobacterium tuberculosis; Trypanosoma cruzi quinoxaline; neglected diseases; Mycobacterium tuberculosis; Trypanosoma cruzi
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MDPI and ACS Style

Ancizu, S.; Moreno, E.; Torres, E.; Burguete, A.; Pérez-Silanes, S.; Benítez, D.; Villar, R.; Solano, B.; Marín, A.; Aldana, I.; Cerecetto, H.; González, M.; Monge, A. Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-N-oxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs. Molecules 2009, 14, 2256-2272.

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