Synthesis of new quinoxaline-2-carboxylate 1,4-dioxide derivatives as anti-Mycobacterium tuberculosis agents.

摘要: Twenty-nine new 6(7)-substituted quinoxaline-2-carboxylate 1,4-dioxide derivatives were synthesized and evaluated for in vitro antituberculosis activity. In general, the activity is significantly affected by substituents on quinoxaline nucleus. It has been observed that presence of a chloro, methyl, or methoxy group position 7 benzene moiety reduces MIC IC50 values. However, principally depends carboxylate group, improving following order:  benzyl > ethyl 2-methoxyethyl allyl tert-butyl. Fourteen compounds have selected macrophage assay, results show 3-methylquinoxaline-2-carboxylate with chlorine (compounds 10 26) unsubstituted 11 27) good antitubercular activity, including macrophages. addition, 28 (the only ones tested up ...