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Advanced targets in Biomedicine

2025 Vol. 1 №2

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Hardunou R. A. Mineyeva I. V.

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.