AZOLE COMPOUNDS, METHOD OF THEIR SYNTHESIS, ANTIFUNGAL PHARMACEUTICAL COMPOSITION AND METHOD OF TREATMENT OF FUNGAL INFECTION

摘要

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention describes azole derivatives of the general formula (I) where R¹ means: 1) C_1-6-alkyl optionally mono- or di-substituted with substitutes taken among: 2-tetrahydrofuryl, C_1-6-acyloxy-group, hydroxy-group, C_1-6-alkoxycarbonyl, benzyloxycarbonyl, carboxy-group, C_1-6-alkanoylamino-group, benzyloxy-C_1-6-alkoxy-group or 1,3- dioxolane-4-yl that in turn can be substituted with C_1-4-alkyl; or 2) 1,3-dioxane-5-yl; n = 0 or 1; R² means hydrogen atom or C_1-6-alkyl; X means halogen atom; Y means halogen atom; Z means -CH₂-CH₂- or N=CH; when Z means the group R⁷ then -CH₂-CH₂- means 3-4 nitrogen-containing 5-membered heterocyclic residue optionally substituted with C_1-6-alkyl that in turn is substituted with C_1-6-acyloxy-group; when Z means the group N= CH- then R⁷ means C_1-6-alkoxy-group substituted with halogen atom. Invention relates to also an antifungal pharmaceutical composition and a method of treatment of fungal infection. Compounds (I) show the increased solubility in water, the improved internal absorption and, therefore, they show good effect in treatment of fungal diseases. EFFECT: improved method of synthesis and treatment, valuable medicinal properties. 10 cl, 7 tbl, 2 dwg, 43 ex