A simple method based on hydrolysis of 2,3-dicyanopyrazinium salts has been used for the
synthesis of the corresponding 5-(hetero)aryl-3-cyano-1-ethyl-2(1H)-pyrazinones. Also, the series of
novel 1-ethyl-5-(hetero)aryl-1,6-dihydropyrazine-2,3-dicarbonitriles have been obtained through reduction
of the same pyrazinium salts with triethylsilane. The obtained compounds proved to be active in
micromolar concentrations in vitro against Mycobacterium tuberculosis H37Rv, Mycobacterium avium,
Mycobacterium terrae, as well as against rifampicin and isoniazid-resistance strains of Mycobacterium
tuberculosis. The data for acute in vivo toxicity in mice have been obtained for these compounds which
appear to be promising antitubercular agents.
Keywords: Pyrazine, 2(1H)-Pyrazinone, antituberculosis activity, tuberculosis, mycobacterium avium, mycobacterium terrae.
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