The hydrolysis of substituted 3-(3-cyanothiophen-2-yl)imino-3H-furan-2-ones was studied. It was found that the reaction proceeds with the opening of the furan ring and the formation of the corresponding 4-oxo-2-(3-cyanothiophen-2-yl)aminobut-2-enoic acids. The antibacterial activity of the obtained compounds against Staphylococcus aureus, Escherichia coli and Candida albicans was studied.

The interaction of 5-arylfuran-2,3-diones with 5,6-R-benzo[ d ]thiazole-2-amines has resulted in 4-aryl- N -(5,6-R-benzo[ d ]thiazol-2-yl)-2-hydroxy-4-oxobut-2-enamides. The products structure has been confirmed by means of IR, NMR, and 1 H NMR spectroscopy as well as mass spectrometry. Analgesic and antimicrobial activities of the prepared compounds have been studied; acute toxicity of the most active compounds has been determined. The relationship between the structure and biological activity of the obtained compounds has been elucidated. The compounds acting comparably or better than the reference drugs have been found.

С целью изучения противомикробной активности синтезированы моно- и бикватернизованные производные дипиридилэтана (этиленов). Исследована противомикробная активность (ПМА) полученных соединений в отношении штаммов грамотрицательной кишечной палочки и грамположительного золотистого стафилококка. Установлена зависимость проявляемой ПМА от природы радикала при атоме азота, положения этано- и этеномостиков между циклами относительно ониевых атомов азота, наличия сопряженной системы между ними. Максимальную ПМА проявляет бромид 1-(N-додецилпиридиний-4-ил)-2-(4-пиридил)этилена в отношении изученных штаммов (3,9 и 2,0 мкг/мл соответственно).

A series of mono-and biquaternized derivatives of dipyridylethanes and dipyridylethylenes has been synthesized and characterized with respect to antimicrobial activity. The new compounds exhibit structure-dependent antimicrobial action on both Gram-negative (E. coli) and Gram-positive (St. aureus) bacterial species. Monoquaternized dipyridylethane and dipyridylethylene derivatives show a higher antimicrobial activity than compounds with two onium nitrogen atoms; derivatives of dipyridylethane are less active than the analogous derivatives of dipyridylethylene. A high antimicrobial activity (MIC ∼ 1 mg/ml) was observed for 1-[N-cetyl-(4-pyridinium)]-2-(4-pyridyl)ethylene.

Synthesis of a small library of compounds containing an aminovinylketone fragment is described. Results of studying their antibacterial activity against S. aureus ATCC 6538-P and E. coli ATCC 25922 are reported.

Synthesis of a small library of compounds containing aminovinylketone fragment is described and results of studying their antibacterial activity against St. aureus ATSS 6538-P and E. coli ATSS 25922 are presented.