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The quaternization reactions of nicotinamide, with different electrophiles: methyl iodide and substituted 2-bromoacetophenones (4-Cl, 4-Br, 4-H, 4-CH3, 4-F, 4-OCH3, 4-Ph, 2-OCH3, 4-NO2) are reported. The preparations were carried out by conventional synthesis and under microwave irradiation in absolute ethanol and acetone. The synthesis performed by microwave dielectric heating significantly improved yield, up to 8 times, and shortened down the reaction time from ca. one day in conventional, to 10–20 min. The structures of the synthesized compounds were confirmed by IR, 1H- and 13C-NMR spectroscopy, mass spectrometry and elemental analysis. The compounds have been screened for antifungal activities against Fusarium oxysporum, Fusarium culmorum, Macrophomina phaseolina and Sclerotinia sclerotiorum at concentrations of 10 µg/mL and 100 µg/mL. Six compounds showed the strong inhibition of mycelium growth at a concentration of 10 µg/mL. All tested compounds revealed the great inhibitory activities against S. sclerotiorum at a concentration of 100 µg/mL.

Indexing p. 1  Editorial Bord p. 1  Guide for Authors p. 3  Manuscript preparation p. 5

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In this study, reactions of quaternization under microwave heating of pyridine, α-picoline, pyridine-4-aldoxime, pyridine-2-aldoxime, nicotinamide, isonicotinamide and pyridoxal oxime with different electrophiles: 2-bromo-4'-nitroacetophenone, 2-amino-4-chloro-methylthiazole hydrochloride, methyl iodide, 1,3-diiodopropane and 1,3-dibromopropane are reported. The synthesis yield by microwave dielectric heating is improved and reaction time shortened compared to conventional heating. The structure of obtained molecules were analyzed and determined by 1D and 2D NMR spectroscopy methods, IR spectroscopy and mass spectrometry. The highest antibacterial activity against two Gram-positive and two Gram-negative bacteria strains has been found for 1-[2-(4-nitrophenyl)-2-oxoethyl]pyridinium bromide (2).

Ten novel isonicotinamide derivatives were prepared by quaternization reactions of isonicotinamide with methyl iodide and nine differently substituted 2-bromoacetophenones under rapid microwave irradiation of 10 minutes. The microwave preparations were significantly faster and with yields higher up to 8 times, than the preparations by conventional method. The structures of synthesized molecules were determined by one-and two-dimensional NMR and IR spectroscopy, mass spectrometry and elemental analysis. Antifungal activity of all compounds was tested in two different concentrations (10 and 100 µg mL -1 ) against Fusarium oxysporum, Fusarium culmorum, Macrophomina phaseolina and Sclerotinia sclerotiorum in vitro. From the antifungal assay it can be seen that the most prepared compounds have moderate to weak activity against M. phaseolina and F. culmorum. A very high inhibitory rate was observed against S. sclerotiorum, 62-87.5 % in concentration of 10 µg mL -1 and 83.7-93.2 % in concentration of 100 µg mL -1 .

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