Synthesis and Evaluation of the Antifungal and Toxicological Activity of Nitrofuran Derivatives

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Vaso, Carolina Orlando ; Pandolfi, Fabiana ; Bila, Niura Madalena ; De Vita, Daniela ; Bortolami, Martina ; Soares Mendes-Giannini, Maria Jose ; Tudino, Valeria ; Costi, Roberta ; Costa-Orlandi, Caroline Barcelos ; Fusco-Almeida, Ana Marisa ; Scipione, Luigi

• Tipo de documento: Artigo Científico
• Fonte: PHARMACEUTICS; v. 14, n. 3, p. 19-pg., 2022-03-01.

Resumo

Fungal diseases affect more than 1 billion people worldwide. The constant global changes, the advent of new pandemics, and chronic diseases favor the diffusion of fungal pathogens such as Candida, Cryptococcus, Aspergillus, Trichophyton, Histoplasma capsulatum, and Paracoccidioides brasiliensis. In this work, a series of nitrofuran derivatives were synthesized and tested against different fungal species; most of them showed inhibitory activity, fungicide, and fungistatic profile. The minimal inhibitory concentration (MIC90) values for the most potent compounds range from 0.48 mu g/mL against H. capsulatum (compound 11) and P. brasiliensis (compounds 3 and 9) to 0.98 mu g/mL against Trichophyton rubrum and T. mentagrophytes (compounds 8, 9, 12, 13 and 8, 12, 13, respectively), and 3.9 mu g/mL against Candida and Cryptococcus neoformans strains (compounds 1 and 5, respectively). In addition, all compounds showed low toxicity when tested in vitro on lung cell lines (A549 and MRC-5) and in vivo in Caenorhabditis elegans larvae. Many of them showed high selectivity index values. Thus, these studied nitrofuran derivatives proved to be potent against different fungal species, characterized by low toxicity and high selectivity; for these reasons, they may become promising compounds for the treatment of mycoses. (AU)

• Processo FAPESP: 20/15586-4 - Estabelecimento de um modelo tridimensional para determinação da eficácia e segurança farmacológica de derivados de nitrofuranos e indólicos e avaliação da infecção de Histoplasma capsulatum
• Beneficiário: Carolina Orlando Vaso
• Modalidade de apoio: Bolsas no Brasil - Doutorado Direto
• Processo FAPESP: 16/11836-0 - SELEÇÃO DE ALVOS TERAPÊUTICOS E/OU BIOMARCADORES A PARTIR DA RESPOSTA TRANSCRICIONAL GLOBAL DA INFECÇÃO DE MACRÓFAGOS ALVEOLARES POR BIOFILMES DE H. capsulatum
• Beneficiário: Ana Marisa Fusco Almeida
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 19/22188-8 - Avaliação da interação de biofilmes mono e dual-espécies de Candida spp e dermatófitos combinada a terapia fotodinâmica com 2-chalcona
• Beneficiário: Níura Madalena Bila
• Modalidade de apoio: Bolsas no Brasil - Doutorado Direto
• Processo FAPESP: 17/18388-6 - O papel do biofilme na patogênese das dermatofitoses e desenvolvimento de estratégias de combate
• Beneficiário: Caroline Barcelos Costa Orlandi
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado