ABSTRACT
Objective To design and synthesize novel triazole antifungal derivatives with 1 ,3 ,4-oxadiazole side chain for the study of antifungal activities. Methods Fourteen title compounds were synthesized via acylation ,aminolysis reaction ,cy-clization ,nucleophilic substitution ,etc. All the compounds were characterized by 1 H NMR ,MS spectra. The in vitro antifun-gal activities were evaluated against six human pathogenic fungi through the micro-broth dilution method. Results The title compounds exhibited strong antifungal activities against all the tested fungi ,especially against Candida albicans. Compounds 10d ,10i , 10l , and 10n were found to be the most effective , with a minimum inhibitory concentration (MIC80 ) of 0.003 9 μg/ml .They are 16-fold more potent than ICZ ( MIC80 0.062 5 μg/ml) and 64-fold more potent than FCZ (MIC80 0.25 μg/ml) .Conclusion The 1 ,3 ,4-oxadiazole side chain could affect the antifungal activities. That could be due to the prop-er incorporation between the 1 ,3 ,4-oxadiazole substituted phenyl ring with the target enzyme.
ABSTRACT
Objective To optimize novel triazole antifungal compounds synthesis of key intermediates.Methods The or-thogonal experimental design is used,emphasizing on four factors including the reaction temperature,the weight ratio of mate-rial,reaction time and solvent on the yield.Results The effect of reaction temperature on the reaction yield is the most signifi-cant,followed by reaction time ;the weight ratio of material and solvent on the yield impact is not obvious.Conclusion The new technology has several advantages and yields up to about 50%,less reactive impurities,easy post processing.
ABSTRACT
Breast cancer has become the main malignant tumors which pose a serious threat to women's health .Selective estrogen receptor modulators ,which served as the effective drug treatment ,have been attracting more attention .Present re‐search progress on the selective estrogen receptor modulators was summarized in this paper .