Heterocyclic-2-carboxylic acid (3-cyano-1,4-di-N-oxidequinoxalin-2-yl)amide derivatives as hits for the development of neglected disease drugs.

Ancizu, S. (Saioa); Moreno-de-Viguri, E. (Elsa); Torres, E. (Enrique); Burguete, A. (Asunción); Pérez-Silanes, S. (Silvia); Benitez, D. (Diego); Raquel; Solano, B. (Beatriz); Marin, A. (Adoración); Aldana, I. (Ignacio); Cerecetto, H. (Hugo); Gonzalez, M. (Mercedes); Monge, A. (Antonio)

Keywords:

Quinoxaline
Neglected diseases
Mycobacterium tuberculosis
Trypanosoma cruz

Issue Date:

2009

Publisher:

MDPI

Publisher Version:

http://www.mdpi.com/journal/molecules

ISSN:

1420-3049

Citation:

Ancizu S, Moreno E, Torres E, Burguete A, Perez-Silanes S, Benitez D, et al. 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 Jun 22;14(6):2256-2272.

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.

URI:

https://hdl.handle.net/10171/23599

Appears in Collections:

DA - CIFA - I+D de medicamentos - Artículos de revistas
DA - Farmacia - Orgánica - Artículos de revista

Files in This Item: