Preliminary antifungal activity assay of selected chlorine‐containing derivatives of xanthone and phenoxyethyl amines

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 metho...

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Published in:Chemical biology & drug design 2018-11, Vol.92 (5), p.1867-1875
Main Authors: Klesiewicz, Karolina, Żelaszczyk, Dorota, Trojanowska, Danuta, Bogusz, Bożena, Małek, Marianna, Waszkielewicz, Anna, Szkaradek, Natalia, Karczewska, Elżbieta, Marona, Henryk, Budak, Alicja
Format: Article
Language:English
Subjects:
amine derivatives
Amines - chemical synthesis
Amines - chemistry
Amines - pharmacology
Antifungal Agents - chemical synthesis
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Arthrodermataceae - drug effects
Aspergillus - drug effects
Chlorine - chemistry
dermatophytes
Microbial Sensitivity Tests
moulds
Structure-Activity Relationship
Trichophyton - drug effects
xanthone derivatives
Xanthones - chemical synthesis
Xanthones - chemistry
Xanthones - pharmacology
yeast
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Summary: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 50 and MIC 90 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 50 and MIC 90 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. The selected chlorine derivatives of xanthone and phenoxyethyl amines were evaluated in vitro against dermatophytes, moulds and yeasts. We observed that only simple amine derivatives of xanthones and phenoxyethyl derivatives of pyridinyl‐ or pyrimidinylpiperazine exhibited promising antifungal activity. The most active compound (4) showed a broad spectrum of activity, being active against all 22 clinical strains tested, with MIC values ranging from 8 to 32 μg/ml.
ISSN:1747-0277
1747-0285
DOI:10.1111/cbdd.13356