2020
DOI: 10.3390/molecules25020345
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Antifungal Styryloquinolines as Candida albicans Efflux Pump Inhibitors: Styryloquinolines are ABC Transporter Inhibitors

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 wit… Show more

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Cited by 17 publications
(7 citation statements)
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References 52 publications
(61 reference statements)
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“…Recently, the activity of four different Styryloquinoline compounds as ABC transport pump inhibitors and the role of the hydroxyl group attached to the quinolone moiety was investigated, the study reveals that the addition of unprotected hydroxyl group at carbon 4 and 8 in the quinolone moiety dramatically increased the antifungal activity against a wild and mutant strain of Candida species. Additionally, the same compound demonstrates a strong synergistic action when combined with fluconazole [46].…”
Section: Discussionmentioning
confidence: 96%
“…Recently, the activity of four different Styryloquinoline compounds as ABC transport pump inhibitors and the role of the hydroxyl group attached to the quinolone moiety was investigated, the study reveals that the addition of unprotected hydroxyl group at carbon 4 and 8 in the quinolone moiety dramatically increased the antifungal activity against a wild and mutant strain of Candida species. Additionally, the same compound demonstrates a strong synergistic action when combined with fluconazole [46].…”
Section: Discussionmentioning
confidence: 96%
“…Other styrylquinolines have been tested against mutant strains of C. albicans . Compound 17i showed great activity against the strain from which the efflux pump gene was deleted, suggesting it is a substrate for the efflux pump, unlike Amphotericin B, which showed constant MIC values for all strains …”
Section: Structural Changes At the 8hq Core Based On The Microorganis...mentioning
confidence: 99%
“…Compound 17i showed great activity against the strain from which the efflux pump gene was deleted, suggesting it is a substrate for the efflux pump, unlike Amphotericin B, which showed constant MIC values for all strains. 108 The antimicrobial SAR of 8HQ derivatives with structural changes at position 2 are summarized in the Figures 21−23. Several modifications were evaluated regarding the antibacterial activity, highlighting aryl groups, alkyl chains, and saturated heterocycles.…”
Section: ■ Introductionmentioning
confidence: 99%
“…While compound 9 offered lower antifungal activity, which could be attributed to the oxygen atom of the ether 20,21 . Whereas the hydroxyl moiety of the compound 3 could be the cause of its antifungal effect 22 .…”
Section: ________________________________________________________________________________________________________________mentioning
confidence: 99%