Antifungal activity of aminoalcohols and diamines against dermatophytes and yeast
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Medicinal Chemistry Research https://doi.org/10.1007/s00044-020-02636-y
ORIGINAL RESEARCH
Antifungal activity of aminoalcohols and diamines against dermatophytes and yeast César A. Caneschi 1 Bruno A. de Oliveira2 Angelina M. de Almeida2 Renata P. do Carmo1 Francislene J. Martins1 Mauro V. de Almeida2 Nádia R. B. Raposo1 ●
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Received: 4 June 2020 / Accepted: 12 September 2020 © Springer Science+Business Media, LLC, part of Springer Nature 2020
Abstract Dermatomycoses are infections caused by fungi and yeasts and the drug treatment is considered expensive and extensive. Researchers are synthesizing new organic compounds in order to obtain more effective molecules that provide reduced adverse effects. Our research group has synthesized and evaluated the biological activities of aminoalcohol and diamine derivatives, which were considered active against human pathogenic fungi. Therefore, the objective of this study was to evaluate the in vitro antifungal activity of aminoalcohols and diamine derivatives against fungi and yeasts that cause dermatomycoses. The minimum inhibitory concentrations (MICs) and the minimum fungicidal concentration (MFC) of aminoalcohol (1–4) and diamine (5–13) derivatives was determined against Trichophyton mentagrophytes, T. rubrum, Epidermophyton floccosum, and Candida albicans according to protocols from the Clinical and Laboratory Standards Institute. All molecules exhibited fungicidal activity against the evaluated fungal strains, with the MIC and MFC ranging between 0.12 and 1000 μg/mL for filamentous fungi and 0.6 and 1250 μg/mL for yeasts. The best activity was attributed to diamines compared to aminoalcohols, with an emphasis on molecules 6 and 7. These results demonstrate the antifungal potential of the evaluated aminoalcohols and diamines against the four primary fungal species that cause dermatomycoses. Graphical Abstract
Keywords Aminoalcohols Diamines Antifungal activity Dermatomycoses ●
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* César A. Caneschi [email protected] 1
Núcleo de Pesquisa e Inovação em Ciências da Saúde (NUPICS), Faculdade de Farmácia, Universidade Federal de Juiz de Fora, Rua José Lourenço Kelmer, s/n, Juiz de Fora, MG 36036-330, Brazil
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Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Rua José Lourenço Kelmer, s/n, Juiz de Fora, MG 36036-330, Brazil
Medicinal Chemistry Research
Introduction Dermatomycoses are superficial infections that can trigger inflammatory conditions and ulcerations [1–5]. This type of mycosis is associated with several predisposing factors, such as climatic conditions, sports activities, prolonged contact with water, lifestyle, immunological status, chronic diseases, and older age [6]. The main etiological agents of these infections are the microorganisms oh the genera Trichophyton, Microsporum, and Epidermophyton, which include the species T. rubrum, T. mentagrophytes, E. floccosum, and M. canis [1, 4–7]. In contrast, the genus Candida comprises opportunistic yeast fungi w
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