Vaso Carolina Orlando, Pandolfi Fabiana, Bila Níura Madalena, De Vita Daniela, Bortolami Martina, Mendes-Giannini Maria José Soares, Tudino Valeria, Costi Roberta, Costa-Orlandi Caroline Barcelos, Fusco-Almeida Ana Marisa, Scipione Luigi
School of Pharmaceutical Science, Universidade Estadual Paulista, Araraquara 14800-903, SP, Brazil.
Department of Scienze di Base e Applicate per l'Ingegneria, Sapienza University of Rome, Via Castro Laurenziano 7, 00185 Rome, Italy.
Pharmaceutics. 2022 Mar 8;14(3):593. doi: 10.3390/pharmaceutics14030593.
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 , , , , and . 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 (MIC) values for the most potent compounds range from 0.48 µg/mL against (compound ) and (compounds and ) to 0.98 µg/mL against and (compounds , , , and , , , respectively), and 3.9 µg/mL against and strains (compounds and , respectively). In addition, all compounds showed low toxicity when tested in vitro on lung cell lines (A549 and MRC-5) and in vivo in 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.
真菌疾病在全球影响着超过10亿人。全球持续的变化、新的大流行病的出现以及慢性病有利于真菌病原体如[此处原文未给出具体病原体名称]的传播。在这项工作中,合成了一系列硝基呋喃衍生物并针对不同真菌物种进行了测试;其中大多数表现出抑制活性、杀真菌和抑菌特性。最有效化合物的最低抑菌浓度(MIC)值范围从针对[此处原文未给出具体真菌名称](化合物[此处原文未给出化合物编号])和[此处原文未给出具体真菌名称](化合物[此处原文未给出化合物编号]和[此处原文未给出化合物编号])的0.48 µg/mL到针对[此处原文未给出具体真菌名称]和[此处原文未给出具体真菌名称]菌株(分别为化合物[此处原文未给出化合物编号]、[此处原文未给出化合物编号]、[此处原文未给出化合物编号]和[此处原文未给出化合物编号]以及[此处原文未给出化合物编号]、[此处原文未给出化合物编号]、[此处原文未给出化合物编号])的0.98 µg/mL,以及针对[此处原文未给出具体真菌名称]和[此处原文未给出具体真菌名称]菌株(分别为化合物[此处原文未给出化合物编号]和[此处原文未给出化合物编号])的3.9 µg/mL。此外,所有化合物在体外对肺细胞系(A549和MRC - 5)以及在体内对[此处原文未给出具体生物名称]幼虫进行测试时均显示出低毒性。它们中的许多显示出高选择性指数值。因此,这些研究的硝基呋喃衍生物被证明对不同真菌物种有效,具有低毒性和高选择性的特点;由于这些原因,它们可能成为治疗真菌病的有前景的化合物。