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

Saioa Ancizu¹  Elsa Moreno¹  Enrique Torres¹  Asunción Burguete¹  Silvia Pérez-Silanes¹  Diego Benítez¹  Raquel Villar¹  Beatriz Solano¹  Adoración Marín¹  Ignacio Aldana¹  Hugo Cerecetto¹  Mercedes González¹ 

[1] ¹Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, C/Irunlarrea s/n, 31008 Pamplona, Spain ²Laboratorio de Química Orgánica, Facultad de Ciencias/Facultad de Química, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay

关键词: quinoxaline;    neglected diseases;    Mycobacterium tuberculosis;    Trypanosoma cruzi;   

DOI  :  10.3390/molecules14062256

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.