8-Hydroxyquinoline-5-sulfonamides are promising antifungal candidates for the topical treatment of dermatomycosis.

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ID: 70137
2019
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Abstract
The purpose of this study was to uncover insights into the mechanism of action of the 8-hydroxyquinoline derivatives PH151 and PH153. In addition, with the future perspective of developing a topical drug for the treatment of candidiasis and dermatophytosis, the antifungal activity of a nanoemulsion formulation containing the most active compound (PH151) is also presented here.Sorbitol Protection Assay and Scanning electron microscopy indicate that the 8-hydroxyquinoline derivatives act on the cell wall of Candida sp. and dermatophytes and they have inhibit the pseudohyphae formation of C. albicans. These findings demonstrate a strong effect of these compounds on C. albicans morphogenesis, which can be considered a potential mode of action for this molecule. Besides, the nanoemulsion formulation MIC values ranged from 0·5 to 4 μg mL demonstrating important antifungal activity when incorporated into a pharmaceutical formulation.Taken together, the results support the potential of these molecules as a promising antifungal candidate for the treatment of candidiasis and dermatophytosis.There is an emerging need to fill the pipeline with new antifungal drugs due to the limitations presented by the currently used drugs. In this study, we have described a novel formulation with a 8-hydroxyquinoline-5-sulfonamide derivative which has presented a great potency providing a finished product. Furthermore, the derivative has shown a selective mechanism of action confirming its potential to be developed as a new drug candidate.
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pippi20198hydroxyquinoline5sulfonamidesjournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Pippi, Bruna;Joaquim, Angélica Rocha;Lopes, William;da Rosa Monte Machado, Gabriella;Zafaneli Bergamo, Vanessa;Giuliani, Laura Minussi;Abegg, Maxwel Adriano;Cruz, Letícia;Vainstein, Marilene Henning;Fuentefria, Alexandre Meneghello;de Andrade, Saulo Fernandes;
Journal Journal of applied microbiology
Year 2019
DOI
10.1111/jam.14545
URL
Keywords
infection pharmaceuticals fungi mechanism of action antimicrobials pseudohyphae

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