FIELD: pharmaceuticals.
SUBSTANCE: invention relates to novel pyrimidine derivative, namely to 3,4-dimethyl-6-(3-pyridyl)-N-phenyl-2-oxo-1,2,3,6-tetrahydropyrimidine-5-carboxamide of formula (1). Compound has antifungal effect against the strain of Candida albicans, which suggests its use in medical practice as antifungal agent. 
. Compound 1 is prepared by reacting a three-component condensation of acetoacetanilide, 3-pyridinecarboxaldehyde, N-methylurea while maintaining the reagents at a temperature of 120–150 °C before the gas evolution ceases and the reaction mixture solidifies, after cooling, the residue is treated with ethanol. Claimed compound is a colorless crystal with Tpl 243–245 °C, soluble in dimethylformamide, acetic acid, when heated – in ethanol, stable during storage. Compound has antifungal activity with a minimum inhibitory concentration of 31.25 mcg/ml with respect to Candida albicans. LD50 when administered intraperitoneally to white mice was 5,640 mg/kg.
EFFECT: compound has antifungal effect.
1 cl, 1 tbl, 1 ex
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Year |
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