Position of CH2CN group in the benzimidazole system determines the activity of hydrogen atoms of CH2 group in condensation reactions. Some of the obtained compounds show high tuberculostatic activity.

Aldehydes↗

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Studies on pyrazine derivatives. Part XIII. synthesis and tuberculostatic activity of some 6-alkyl-amino- and 6-dialkylhydrazinopyrazine-2-carboxylic acids derivatives.

6-RNH- and 6-R2NNH-pyrazine-2-carbothioamides 1--3, 5, 6, 9 and 14 were obtained from 2-cyano-6-chloropyrazine. In the in vitro screening the thioamides were active against Myc. tuber. H37Rv at the conc. range of 15.6--250 microgram/cm3. The most active thioamides 1 and 8, however, do not act in experimental tuberculosis in guinea pigs.

Amines↗

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Studies on pyrazine derivatives. Part III. The synthesis and tuberculostatic activity of 6-(N-methyl-amino2)-pyrazine-2-carboxylic acid derivatives.

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Antitubercular Agents↗

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Synthesis of some 2-aminonicotinic acid derivatives.

The nucleophilic exchange of chlorine atom in 2-chloro-3-cyanopyridine with morpholine, piperidine and pyrrolidine was carried out. Acids, amides, thioamides, esters and hydrazides were derived from the obtained compounds (Fig. 1). Some of these compounds showed only moderate tuberculostatic activity.

Chemical Phenomena↗

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Investigations of pyrazine derivatives. Part IV. Synthesis and tuberculostatic activity of some 6-alkoxypyrazine-2-carboxylic acids.

By alcoholysis of 2-cyjano-6-chloropyrazine corresponding 6-alkoxypyrazine-2-imidoesters (1,6,11,16) were formed, which were then transformed in esters and amides of 6-alkoxypyrazine-2-carboxylic acids. Some of these compounds show a weak tuberculostatic activity.

Antitubercular Agents↗