Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus
| Autor: | Fei Xie, Yong-Sheng Jin, Xiaoyun Chai, Tingjunhong Ni, Dazhi Zhang, Yuanying Jiang, Shichong Yu, Zichao Ding, Ting Wang, Yumeng Hao |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Antifungal Agents
Clinical Biochemistry Triazole Pharmaceutical Science Microbial Sensitivity Tests 01 natural sciences Biochemistry Microbiology Aspergillus fumigatus Fungal Proteins Sterol 14-Demethylase Structure-Activity Relationship chemistry.chemical_compound Drug Resistance Fungal Catalytic Domain Candida albicans Drug Discovery medicine Structure–activity relationship Fluconazole Molecular Biology Voriconazole Binding Sites biology 010405 organic chemistry Organic Chemistry Triazoles biology.organism_classification In vitro 0104 chemical sciences Molecular Docking Simulation 010404 medicinal & biomolecular chemistry chemistry Drug Design Molecular Medicine Albaconazole medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 30:126951 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2020.126951 |
| Popis: | The incidence of invasive fungal infections has dramatically increased for several decades. In order to discover novel antifungal agents with broad spectrum and anti-Aspergillus efficacy, a series of novel triazole derivatives containing 1,2,3-benzotriazin-4-one was designed and synthesized. Most of the compounds exhibited stronger in vitro antifungal activities against tested fungi than fluconazole. Moreover, 6m showed comparable antifungal activity against seven pathogenic strains as voriconazole and albaconazole, especially against Aspergillus fumigatus (MIC = 0.25 μg/ml), and displayed moderate antifungal activity against fluconazole-resistant strains of Candida albicans. A clear SAR study indicated that compounds with groups at the 7-position resulted in novel antifungal triazoles with more effectiveness and a broader-spectrum. |
| Databáze: | OpenAIRE |
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