3 research outputs found
Quinoxaline 1,4-di-N-oxide and the Potential for Treating Tuberculosis
New drugs active against drug-resistant tuberculosis are urgently needed to extend the range of TB treatment options to cover drug resistant infections. Quinoxaline derivatives show very interesting biological properties (antibacterial, antiviral, anticancer, antifungal, antihelmintic, insecticidal) and evaluation of their medicinal chemistry is still in progress. In this review we report the properties and the recent developments of quinoxaline 1,4-di-N-oxide derivatives as potential anti-tuberculosis agents. Specific agents are reviewed that have excellent antitubercular drug properties, are active on drug resistant strains and non-replicating mycobacteria. The properties of select analogs that have in vivo activity in the low dose aerosol infection model in mice will be reviewed
Quinoxaline 1,4-di-N-oxide and the Potential for Treating Tuberculosis
New drugs active against drug-resistant tuberculosis are urgently needed to extend the range of TB treatment options to cover drug resistant infections. Quinoxaline derivatives show very interesting biological properties (antibacterial, antiviral, anticancer, antifungal, antihelmintic, insecticidal) and evaluation of their medicinal chemistry is still in progress. In this review we report the properties and the recent developments of quinoxaline 1,4-di-N-oxide derivatives as potential anti-tuberculosis agents. Specific agents are reviewed that have excellent antitubercular drug properties, are active on drug resistant strains and non-replicating mycobacteria. The properties of select analogs that have in vivo activity in the low dose aerosol infection model in mice will be reviewed
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 IC50 values in the same order
as the anti-chagasic drug, nifurtimox