Molecules (2019)
Update date:2022-07-29
Topics: Data Analysis Structure-Activity Relationship (SAR) Analysis Purification and characterization Materials and Reagents Safety and Toxicity Assessment Publication and Further Research Antifungal Activity Evaluation Synthesis of Nicotinamide Derivatives
Siber, Tamara
Bu?i?, Valentina
Zobund?ija, Dora
Roca, Sun?ica
Viki?-Topi?, Dra?en
Vrande?i?, Karolina
Ga?o-Soka?, Dajana
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.
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Doi:10.1002/chem.201901268
(2019)Doi:10.1002/chem.200800040
(2008)Doi:10.1021/acs.organomet.0c00816
(2021)Doi:10.1002/ejic.200700597
(2007)Doi:10.1021/jo0705061
(2007)Doi:10.1016/S0040-4039(97)10181-2
(1997)