Heterocyclic-2-carboxylic acid (3-cyano-1,4-di-N-oxidequinoxalin-2-yl)amide derivatives as hits for the development of neglected disease drugs.
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 IC(50) values in the same order as the anti-chagasic drug, nifurtimox.
Ancizu
Saioa
S
Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada, University of Navarra, C/Irunlarrea s/n, 31008 Pamplona, Spain.
Moreno
Elsa
E
Torres
Enrique
E
Burguete
Asunción
A
Pérez-Silanes
Silvia
S
Benítez
Diego
D
Villar
Raquel
R
Solano
Beatriz
B
Marín
Adoración
A
Aldana
Ignacio
I
Cerecetto
Hugo
H
González
Mercedes
M
Monge
Antonio
A
D000818:Animals; D000995:Antitubercular Agents / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011810:Quinoxalines / Q000737:chemistry* / Q000494:pharmacology*; D012293:Rifampin; D014345:Trypanosoma / Q000187:drug effects
D000995:Antitubercular Agents; D011810:Quinoxalines; D012293:Rifampin