The synthesis and synergistic antifungal effects of chalcones against drug resistant Candida albicans
Autor: | Yuan-Hua Wang, Yong-Sheng Jin, Yuanying Jiang, Huai-Huai Dong, Jie Wang, Fei Zhao, Fang Yan |
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Rok vydání: | 2016 |
Předmět: |
0301 basic medicine
Antifungal Chalcone Antifungal Agents medicine.drug_class 030106 microbiology Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Drug resistance Pharmacology 01 natural sciences Biochemistry Structure-Activity Relationship 03 medical and health sciences Minimum inhibitory concentration chemistry.chemical_compound Chalcones Drug Resistance Fungal Candida albicans Drug Discovery medicine Structure–activity relationship Molecular Biology Dose-Response Relationship Drug Molecular Structure biology 010405 organic chemistry Chemistry Organic Chemistry biology.organism_classification In vitro 0104 chemical sciences Molecular Medicine Fluconazole medicine.drug |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 26:3098-3102 |
ISSN: | 0960-894X |
DOI: | 10.1016/j.bmcl.2016.05.013 |
Popis: | To identify effective and low toxicity synergistic antifungal compounds, 24 derivatives of chalcone were synthesized to restore the effectiveness of fluconazole against fluconazole-resistant Candida albicans. The minimal inhibitory concentration (MIC80) and the fractional inhibitory concentration index (FICI) of the antifungal synergist fluconazole were measured against fluconazole-resistant Candida albicans. This was done via methods established by the clinical and laboratory standards institute (CLSI). Of the synthesized compounds, 2'-hydroxy-4'-methoxychalcone (8) exhibited the most potent in vitro (FICI=0.007) effects. The structure activity relationship of the compounds are then discussed. |
Databáze: | OpenAIRE |
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