FIELD: chemistry.
SUBSTANCE: invention relates to synthesis of biologically active analogues of natural compounds, specifically to production of a new representative of nitrogen-containing derivatives of fusidic acid - (2Z)-2-[(3β,4α,8α,11α,14β,16β)-16-(acetyloxy)-3-({3-[(4-aminobutyl)amino]propyl}amino)-11-hydroxy-4,8,10,14-tetramethyl-gonan-17-ylidene]-6-methylhept-5-enoic acid (compound (1)), having antibacterial activity on Staphylococcus aureus (MRSA) and inhibiting growth of a fungal culture of Cryptococcus neoformans. Compound (1) is obtained based on the corresponding dioxo-derivative of fusidic acid by reacting with 6 equivalents of spermidine in the presence of titanium (IV) isopropoxide in dry methanol medium while stirring for 2 hours. Output of compound (1) is 90 %.
EFFECT: compound (1) shows fungicidal activity with respect to the pathogenic fungal culture of Cryptococcus neoformans with low toxicity and has minimal haemolytic action at the maximum tested concentration.
2 cl, 2 tbl, 1 ex
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Author |
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