Synthesis of new 3,4-dihydropyrimidin-2(1h)-ones: optimisation of synthesis conditions and analysis of antifungal activity of the obtained compounds
- DOI
- 10.5922/ATB-2025-1-2-6
- Pages
- 89-105
3,4-dihydropyrimidin-2(1H)-ones
Biginelli multicomponent reaction
aliphatic and cyclopropane-containing aldehydes
europium (III) chloride
indium (III) chloride
yttrium (III) chloride
ytterbium (III) chloride
PerMM service
Pass Online service
in silico analysis
Yarrowia lipolytica
Abstract
This paper for the first time presents an efficient method for the synthesis of 3,4-dihydropyrimidin-2(1H)-ones (3,4-DHPMs) bearing aliphatic and cyclopropane-containing aldehyde residues, using europium(III) chloride hexahydrate as a catalyst in the Biginelli multicomponent reaction (MCR). A high permeability through the phospholipid bilayer and the potential for passive diffusion facilitating participation in intracellular interactions were determined. A preliminary evaluation of the antifungal properties of the obtained compounds against a range of fungal species was carried out using in silico
methods. Experiments on the effect of 3,4-dihydropyrimidinones on the growth of Yarrowia lipolytica yeast showed no acute toxicity of the tested compounds within the micromolar concentration range.
methods. Experiments on the effect of 3,4-dihydropyrimidinones on the growth of Yarrowia lipolytica yeast showed no acute toxicity of the tested compounds within the micromolar concentration range.