Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi
| Autor: | Dongmei Zhao, Lei Liu, Tianxiao Wu, Hengxian Cui, Hong Jiang, Yuxin Zhang, Maosheng Cheng, Yang Zheng, Yin Sun, Xin Su, Song Li, Liyu Zhao, Wenbo Yin |
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| Rok vydání: | 2021 |
| Předmět: |
Antifungal
Antifungal Agents medicine.drug_class Antifungal drugs Microbial Sensitivity Tests Thiophenes Microbiology Structure-Activity Relationship Drug Resistance Fungal Drug Discovery Candida albicans medicine Humans Fluconazole Pharmacology biology Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Biofilm General Medicine biology.organism_classification Fungicides Industrial Fungicide Design synthesis Drug Design Fluconazole resistant |
| Zdroj: | European journal of medicinal chemistry. 225 |
| ISSN: | 1768-3254 |
| Popis: | A series of 5-phenylthiophene derivatives with novel structures were designed and synthesized to combat the increasing incidence of susceptible and drug-resistant fungal infections. The antifungal activity of the synthesized compounds was assessed against seven susceptible strains and six fluconazole-resistant strains. It is especially encouraging that compounds 17b and 17f displayed significant antifungal activities against all tested strains. Furthermore, the potent compounds 17b and 17f could prevent the formation of fungi biofilms and 17f displayed satisfactory fungicidal activity. Preliminary mechanistic studies showed that the potent antifungal activity of compound 17f stemmed from inhibition of C. albicans CYP51. In addition, Compounds 17b and 17f were almost nontoxic to mammalian A549, MCF-7, and THLE-2 cells. These results strongly suggested that compounds 17b and 17f are promising as novel antifungal drugs. |
| Databáze: | OpenAIRE |
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