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

杂环-2-羧酸(3-氰基-1,4-二-N-氧化物喹喔啉-2-基)酰胺衍生物作为被忽视疾病药物开发的成功案例

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作者:Saioa Ancizu, Elsa Moreno, Enrique Torres, Asunción Burguete, Silvia Pérez-Silanes, Diego Benítez, Raquel Villar, Beatriz Solano, Adoración Marín, Ignacio Aldana, Hugo Cerecetto, Mercedes González, Antonio Monge

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 IC(50) values in the same order as the anti-chagasic drug, nifurtimox.

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