Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Department of Bioorganic Chemistry, Chair of Organic Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, Kraków, Poland.
Chem Biol Drug Des. 2018 Nov;92(5):1867-1875. doi: 10.1111/cbdd.13356. Epub 2018 Jul 4.
The aim of this study was to evaluate antifungal activity in a diverse group of chlorine-containing xanthone and phenoxyethyl amine derivatives - and to select the most promising compounds for further studies. The antifungal efficacy of 16 compounds was tested with qualitative and quantitative methods against both reference and clinical strains of dermatophytes, moulds and yeasts. The disc-diffusion method has demonstrated that from 16 tested compounds, 7 possess good antifungal activity against dermatophytes and/or moulds while none of them has shown good efficacy against yeasts or bacterial strains. The most active compounds (2, 4, 10, 11, 12, 15, 16) were tested quantitatively by broth dilution method to obtain MIC values. The MIC values against dermatophytes ranged from 8 to 64 μg/ml. Compound 2 was the most active one against dermatophytes (MIC and MIC were 8 μg/ml). The MIC values for moulds ranged from 16 to 256 μg/ml. Compound 4 was the most active one against moulds, with MIC and MIC values amounting to 32 μg/ml. Among the tested compounds, compound 4 (derivative of xanthone) was the most active one and expressed good antifungal efficacy against clinical strains of dermatophytes and moulds. However, another xanthone derivative (compound 2) was the most active and selective against dermatophytes.
本研究旨在评估含氯黄烷酮和苯氧乙胺衍生物的抗真菌活性，并选择最有前途的化合物进行进一步研究。采用定性和定量方法，对 16 种化合物对皮肤癣菌、霉菌和酵母菌的参考株和临床株进行了抗真菌功效测试。纸片扩散法表明，在 16 种测试化合物中，有 7 种对皮肤癣菌和/或霉菌具有良好的抗真菌活性，而它们对酵母菌或细菌株均无良好的疗效。最具活性的化合物（2、4、10、11、12、15、16）通过肉汤稀释法进行定量测试，以获得 MIC 值。这些化合物对皮肤癣菌的 MIC 值范围为 8 至 64μg/ml。化合物 2 对皮肤癣菌的活性最强（MIC 和 MIC 分别为 8μg/ml）。对霉菌的 MIC 值范围为 16 至 256μg/ml。化合物 4 对霉菌的活性最强，MIC 和 MIC 值分别为 32μg/ml。在所测试的化合物中，化合物 4（黄烷酮衍生物）对临床皮肤癣菌和霉菌株的抗真菌效果最好。然而，另一种黄烷酮衍生物（化合物 2）对皮肤癣菌的活性和选择性最强。
