Quinolines derivatives as promising new antifungal candidates for the treatment of candidiasis and dermatophytosis

喹啉衍生物作为治疗念珠菌病和皮肤癣菌病的有希望的新型抗真菌药物

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作者:Gabriella da Rosa Monte Machado, Denise Diedrich, Thaís Carine Ruaro, Aline Rigon Zimmer, Mário Lettieri Teixeira, Luís Flávio de Oliveira, Mickael Jean, Pierre Van de Weghe, Saulo Fernandes de Andrade, Simone Cristina Baggio Gnoatto, Alexandre Meneghello Fuentefria

Abstract

Fungal infections have emerged as a current serious global public health problem. The main problem involving these infections is the expansion of multidrug resistance. Therefore, the prospection of new compounds with efficacy antifungal becomes necessary. Thus, this study evaluated the antifungal profile and toxicological parameters of quinolines derivatives against Candida spp. and dermatophyte strains. As a result, a selective anti-dermatophytic action was demonstrated by compound 5 (geometric means (GM = 19.14 μg ml-1)). However, compounds 2 (GM = 50 μg ml-1) and 3 (GM = 47.19 μg ml-1) have presented only anti-Candida action. Compounds 3 and 5 did not present cytotoxic action. Compound 5 did not produce dermal and mucosal toxicity. In addition, this compound showed the absence of genotoxic potential, suggesting safety for topical and systemic use. Quinolines demonstrated a potent anti-dermatophytic and anti-yeast action. Moreover, compound 5 presented an excellent toxicological profile, acting as a strong candidate for the development of a new effective and safe compound against dermatophytosis of difficult treatment.

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