Abstract
In this paper new quinoxaline derivatives with different substituents in positions 3, 6, 7 and 8 are reported. Their biological activities against Mycobacterium tuberculosis have been assessed and most of the 1,4-di-N-oxide derivatives have been shown to strongly inhibit the bacteria growth in the first in vitro screening. One of these N-oxides (4) is a promising candidate due to its good Selectivity Index (7.95). On the other hand, those compounds without N-oxide moieties showed no or very low activity (growth inhibition: 17% and 39%).
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Antineoplastic Agents / pharmacology
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Antitubercular Agents / chemical synthesis*
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Antitubercular Agents / pharmacology*
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Chlorocebus aethiops
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Indicators and Reagents
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Macrophages / drug effects
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Macrophages / microbiology
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Magnetic Resonance Spectroscopy
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Microbial Sensitivity Tests
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Mycobacterium tuberculosis / drug effects*
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Nitriles / chemical synthesis*
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Nitriles / pharmacology*
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Quinoxalines / chemical synthesis*
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Quinoxalines / pharmacology*
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Spectrophotometry, Infrared
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Spectrophotometry, Ultraviolet
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Vero Cells
Substances
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Antineoplastic Agents
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Antitubercular Agents
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Indicators and Reagents
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Nitriles
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Quinoxalines
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quinoxaline-2-carbonitrile
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quinoxaline-2-carbonitrile 1,4-di-N-oxide