Autor(es):
Vaso, Carolina Orlando [UNESP] ; Pandolfi, Fabiana ; Bila, Níura Madalena [UNESP] ; De Vita, Daniela ; Bortolami, Martina ; Mendes-Giannini, Maria José Soares [UNESP] ; Tudino, Valeria ; Costi, Roberta ; Costa-Orlandi, Caroline Barcelos [UNESP] ; Fusco-Almeida, Ana Marisa [UNESP] ; Scipione, Luigi
Data: 2022
Identificador Persistente: http://hdl.handle.net/11449/234270
Origem: Oasisbr
Assunto(s): Antifungal activity; Broad-spectrum antifungal; Caenorhabditis elegans larvae; Candida sp; Cryptococcus neoformans; Histoplasma capsulatum; Nitrofuran derivates; Paracoccidioides brasiliensis; Trichophyton mentagrophytes; Trichophyton rubrum
Descrição
Made available in DSpace on 2022-05-01T15:30:01Z (GMT). No. of bitstreams: 0 Previous issue date: 2022-03-01
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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 μg/mL against H. capsulatum (compound 11) and P. brasiliensis (compounds 3 and 9) to 0.98 μg/mL against Trichophyton rubrum and T. mentagrophytes (compounds 8, 9, 12, 13 and 8, 12, 13, respectively), and 3.9 μg/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.
School of Pharmaceutical Science Universidade Estadual Paulista, SP
Department of Scienze di Base e Applicate per l’Ingegneria Sapienza University of Rome, Via Castro Laurenziano 7
Department of Environmental Biology Sapienza University of Rome, Piazzale Aldo Moro 5
Department of Chimica e Tecnologia del Farmaco Sapienza University of Rome, Piazzale Aldo Moro
Department of Chemistry and Technology of Drug Instituto Pasteur Fondazione Cenci Bolognetti Sapienza University of Rome, Piazzale Aldo Moro 5
School of Pharmaceutical Science Universidade Estadual Paulista, SP
CAPES: 001
CNPq: 134559/2018-5
CNPq: 142049/2019-0
FAPESP: 16/11836-0
FAPESP: 2017/18388-6
FAPESP: 2019/22188-8
FAPESP: 2020/15586-4
CAPES: 88887.500765/2020-00
