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-...
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| Format: | Article |
| Language: | English |
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MDPI AG
2009-06-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/14/6/2256/ |
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doaj-8d9d3655abf14c9a9b0b3f6aba7ace0a2020-11-25T00:52:26ZengMDPI AGMolecules1420-30492009-06-011462256227210.3390/molecules14062256Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-N-oxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease DrugsAntonio MongeMercedes GonzálezHugo CerecettoBeatriz SolanoIgnacio AldanaAdoración MarínRaquel VillarDiego BenítezSilvia Pérez-SilanesAsunción BurgueteSaioa AncizuElsa MorenoEnrique TorresNeglected 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. http://www.mdpi.com/1420-3049/14/6/2256/quinoxalineneglected diseasesMycobacterium tuberculosisTrypanosoma cruzi |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Antonio Monge Mercedes González Hugo Cerecetto Beatriz Solano Ignacio Aldana Adoración Marín Raquel Villar Diego Benítez Silvia Pérez-Silanes Asunción Burguete Saioa Ancizu Elsa Moreno Enrique Torres |
| spellingShingle |
Antonio Monge Mercedes González Hugo Cerecetto Beatriz Solano Ignacio Aldana Adoración Marín Raquel Villar Diego Benítez Silvia Pérez-Silanes Asunción Burguete Saioa Ancizu Elsa Moreno Enrique Torres 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 quinoxaline neglected diseases Mycobacterium tuberculosis Trypanosoma cruzi |
| author_facet |
Antonio Monge Mercedes González Hugo Cerecetto Beatriz Solano Ignacio Aldana Adoración Marín Raquel Villar Diego Benítez Silvia Pérez-Silanes Asunción Burguete Saioa Ancizu Elsa Moreno Enrique Torres |
| author_sort |
Antonio Monge |
| title |
Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-N-oxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs |
| title_short |
Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-N-oxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs |
| title_full |
Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-N-oxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs |
| title_fullStr |
Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-N-oxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs |
| title_full_unstemmed |
Heterocyclic-2-carboxylic Acid (3-Cyano-1,4-di-N-oxidequinoxalin-2-yl)amide Derivatives as Hits for the Development of Neglected Disease Drugs |
| title_sort |
heterocyclic-2-carboxylic acid (3-cyano-1,4-di-n-oxidequinoxalin-2-yl)amide derivatives as hits for the development of neglected disease drugs |
| publisher |
MDPI AG |
| series |
Molecules |
| issn |
1420-3049 |
| publishDate |
2009-06-01 |
| description |
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. |
| topic |
quinoxaline neglected diseases Mycobacterium tuberculosis Trypanosoma cruzi |
| url |
http://www.mdpi.com/1420-3049/14/6/2256/ |
| work_keys_str_mv |
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