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

• Published in: Brazilian journal of microbiology Vol. 51; no. 4; pp. 1691 - 1701
• Main Authors: da Rosa Monte Machado, Gabriella, Diedrich, Denise, Ruaro, Thaís Carine, Zimmer, Aline Rigon, Lettieri Teixeira, Mário, de Oliveira, Luís Flávio, Jean, Mickael, Van de Weghe, Pierre, de Andrade, Saulo Fernandes, Baggio Gnoatto, Simone Cristina, Fuentefria, Alexandre Meneghello
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.12.2020; Sociedade Brasileira de Microbiologia
• Subjects: Biomedical and Life Sciences; Chemical Sciences; Clinical Microbiology - Research Paper; Food Microbiology; Life Sciences; Medical Microbiology; Microbial Ecology; Microbial Genetics and Genomics; Microbiology; Mycology; Antifungal potential; Quinoline derivatives; Fungal resistance; Dermatophyte; Candida
• ISSN: 1517-8382; 1678-4405
• DOI: 10.1007/s42770-020-00348-4

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.