Selective activity against Mycobacteriumtuberculosis of new quinoxaline 1,4-di-N-oxides.
Bioorg Med Chem
; 17(1): 385-9, 2009 Jan 01.
Article
en En
| MEDLINE
| ID: mdl-19058970
ABSTRACT
New series of 3-phenylquinoxaline 1,4-di-N-oxide with selective activity against Mycobacterium tuberculosis have been prepared and evaluated. Thirty-four of the seventy tested compounds showed an MIC value less than 0.2 microg/mL, a value on the order of the MIC of rifampicin. Furthermore, 45% of the evaluated derivatives showed a good in vitro activity/toxicity ratio. The most active and selective compounds carry a fluorine atom in the quinoxaline 7-position or in the phenyl substituent para-position. In conclusion, the potency, low cytotoxicity and selectivity of these compounds make them valid lead compounds for synthesizing new analogues, particularly compound 7-methyl-3-(4'-fluoro)phenylquinoxaline-2-carbonitrile 1,4-di-N-oxide (MIC <0.2 microg/mL and SI > 500).
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Quinoxalinas
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Mycobacterium tuberculosis
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Antituberculosos
Límite:
Humans
Idioma:
En
Año:
2009
Tipo del documento:
Article