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

Autor: da Rosa Monte Machado G; Postgraduate Program in Agricultural Microbiology and Environment, Federal University of Rio Grande do Sul, Sarmento Leite n° 500, Farroupilha, Porto Alegre, RS, 90050-170, Brazil. gabbirosam@gmail.ocom.; Laboratory of Applied Mycology - Faculty of Pharmacy, Federal University of Rio Grande do Sul, Porto Alegre, Brazil. gabbirosam@gmail.ocom., Diedrich D; Postgraduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, Avenue Ipiranga, n° 2752 - Azenha, Porto Alegre, RS, 90610-000, Brazil., Ruaro TC; Postgraduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, Avenue Ipiranga, n° 2752 - Azenha, Porto Alegre, RS, 90610-000, Brazil., Zimmer AR; Postgraduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, Avenue Ipiranga, n° 2752 - Azenha, Porto Alegre, RS, 90610-000, Brazil., Lettieri Teixeira M; Pharmacology Laboratory, Federal Catarinense Institute, Highway SC 283 - Fragosos, Concórdia, SC, 89703-720, Brazil., de Oliveira LF; Cell Toxicology Research Laboratory, Federal University of Pampa, BR 472 - Km 585, Uruguaiana, RS, 97501-970, Brazil., Jean M; Natural Products Syntheses and Medicinal Chemistry Laboratory, Rennes University 1, Street du Thabor, 35000, Rennes, France., Van de Weghe P; Natural Products Syntheses and Medicinal Chemistry Laboratory, Rennes University 1, Street du Thabor, 35000, Rennes, France., de Andrade SF; Postgraduate Program in Agricultural Microbiology and Environment, Federal University of Rio Grande do Sul, Sarmento Leite n° 500, Farroupilha, Porto Alegre, RS, 90050-170, Brazil.; Postgraduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, Avenue Ipiranga, n° 2752 - Azenha, Porto Alegre, RS, 90610-000, Brazil., Baggio Gnoatto SC; Postgraduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, Avenue Ipiranga, n° 2752 - Azenha, Porto Alegre, RS, 90610-000, Brazil., Fuentefria AM; Postgraduate Program in Agricultural Microbiology and Environment, Federal University of Rio Grande do Sul, Sarmento Leite n° 500, Farroupilha, Porto Alegre, RS, 90050-170, Brazil.; Postgraduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, Avenue Ipiranga, n° 2752 - Azenha, Porto Alegre, RS, 90610-000, Brazil.
Jazyk: angličtina
Zdroj: Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] [Braz J Microbiol] 2020 Dec; Vol. 51 (4), pp. 1691-1701. Date of Electronic Publication: 2020 Jul 31.
DOI: 10.1007/s42770-020-00348-4
Abstrakt: 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.
Databáze: MEDLINE
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