Abstract
Styrylquinolines are heterocyclic compounds that are known for their antifungal and antimicrobial activity. Metal complexation through hydroxyl groups has been claimed to be a plausible mechanism of action for these types of compounds. A series of novel structures with protected hydroxyl groups have been designed and synthesized to verify the literature data. Their antifungal activity against wild-type Candida albicans strain and mutants with silenced efflux pumps activity has been determined. Combinations with fluconazole revealed synergistic interactions that were dependent on the substitution pattern. These results open a new route for designing active antifungal agents on a styrylquinoline scaffold.
Highlights
Invasive mycoses are an important public health problem, especially for immunosuppressed patient
Candida albicans is the one that is most often associated with serious invasive fungal infections, and it is responsible for 8–10% of the cases with a high mortality rate (30–80% depending on the patient) [1]
In hydrolysis and the modified methods that are typically used for styrylquinoline synthesis as is hydrolysis and the modified methods that are typically used for styrylquinoline synthesis as is depicted
Summary
Invasive mycoses are an important public health problem, especially for immunosuppressed patient. Other drugs from the conazoles group, like fluconazole (FLC), have rather limited use due to the fact of resistance Another drug with a wide spectrum of activity is amphotericin B (AmB). One example is the overexpression of the drug transporters (e.g., ATP binding cassette (ABC) pumps—Candida drug resistance (Cdr1p and Cdr2p) This mechanism is not very specific; ABC transporters have the ability to export many structurally dissimilar compounds, for instance, azoles, among others [7]. Their activity non-specific and covered a strains These initial examples were later developed into more sophisticated molecules that had a more broad range of fungal strains. These initial examples were later developed into more sophisticated specific mechanism action.
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