Basic Information
ID: ALA4680171
Journal: Eur J Med Chem
Title: Oxadiazolylthiazoles as novel and selective antifungal agents.
Authors: Hagras M,Salama EA,Sayed AM,Abutaleb NS,Kotb A,Seleem MN,Mayhoub AS
Abstract: Studying the structure-activity relationships (SAR) of oxadiazolylthiazole antibiotics unexpectedly led us to identify ethylenediamine- and propylenediamine-analogs as potential antimycotic novel lead structures. Replacement of the ethylenediamine moiety for the lead compound 7 with cis-diaminocyclohexyl group (compound 18) significantly enhanced the antifungal activity. In addition to the high safety margin of 18 against mammalian cells, it showed highly selective broad-spectrum activity against fungal cells without inhibiting the human normal microbiota. The antifungal activity of 18 was investigated against 20 drug-resistant clinically important fungi, including Candida species, Cryptococcus, and Aspergillus fumigatus strains. In addition to the low MIC values that mostly ranged between 0.125 and 2.0 μg/mL, compound 18 outperformed fluconazole in disrupting mature Candida biofilm.
CiteXplore: 31962263
DOI: 10.1016/j.ejmech.2020.112046
Patent ID: ┄
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