Studies on pyrazine derivatives--XXXIV. Synthesis and tuberculostatic activity of alpha-oxo ketene dithioacetals pyrazine derivatives.

The alpha-oxo ketene dithioacetalic derivatives (2a-e) were obtained by the reaction of 2-acetylpyrazine (1) with CS2 and appropriate mono- or dihalogeno-compound. An action of the primary amines and diamines upon 3,3-di(methylsulphanyl)-1-(2-pyrazinyl)-2-propen-1-one (2a) yielded 3-(alkylamino)-3-(methylsulphanyl)-1-(2-pyrazinyl)-2-propen-1-on e (3a-g), 1-(2-pyrazinyl)-2-tetrahydro-1H-2-imidazolyliden-1-ethanone (3h) and the 2-hexahydro-2-pyrimidinyliden-1-(2-pyrazinyl)-1-ethanone derivatives (3i-j), respectively. Tuberculostatic activity of the studied compounds was found to be low except the compound 2b (MIC 192-62 micrograms/cm3; MIC 210-31 micrograms/cm3).

Studies on pyrazine derivatives. XXXIII. Synthesis and tuberculostatic activity of 1-[1-(2-pyrazinyl)-ethyl]-4-N-substituted thiosemicarbazide derivatives.

Hydrogenation of 4-N-substituted thiosemicarbazonic acid acetylpyrazine derivatives with NaBH4 in dry ethanol led to seventeen new compounds. The in vitro tuberculostatic activity investigations of the 15 synthesized compound were carried out. MIC few of i.

Synthesis and some reactions of 2-acetylimidazo[4,5-b]pyridine. Antituberculotic activity of the obtained compounds.

2-Acetylimidazo[4,5-b]pyridine was prepared and its reactions with some aromatic amines and sulfur (Willgerodt-Kindler reaction), some aromatic aldehydes, some carboxylic acid hydrazides as well as thiourea were investigated. New imidazo[4,5-b]pyridine derivatives with different substituents in 2-position (N-arylthioamides, imines, alpha, beta-unsaturated ketones, hydrazido-hydrazones and aminothiazole) were obtained. Most of the synthesized compounds were tested in vitro for their antituberculotic activity.

Studies on pyrazine derivatives. XXXII. Synthesis and tuberculostatic activity of acetylpyrazine thiosemicarbazone derivatives.

Syntheses of 4-N-substituted thiosemicarbazoic acetylpyrazine derivatives have been described. The in vitro microbiological investigations of the 25 synthesized compound were carried out.

Some reactions of 2-cyanomethylimidazo[4,5-b]pyridine with isothiocyanates. Antituberculotic activity of the obtained compounds.

Some reactions of 2-cyanomethylimidazo[4,5-b]pyridine with isothiocyanates were carried out. New derivatives of imidazo[4,5-b]pyridine with different substituents in 2-position and derivatives of the new thiazolo-pyrido-imidazo-pyrimidine ring system were synthesized. Most of the obtained compounds were tested in vitro for their antituberculotic activity.