Synthesis and antifungal evaluation of chalcone derivatives combined with fluconazole against drug-resistant <i>Candida albicans</i>

SHEN Yunhong; CHEN Hongjie; MAO Zewei; HUANG Zhengxiao; HU Chunyan

doi:10.11665/j.issn.1000-5048.2023041002

Journal of China Pharmaceutical University > 2023 > 54(5): 564-568. > DOI: 10.11665/j.issn.1000-5048.2023041002

SHEN Yunhong, CHEN Hongjie, MAO Zewei, HUANG Zhengxiao, HU Chunyan. Synthesis and antifungal evaluation of chalcone derivatives combined with fluconazole against drug-resistant Candida albicans[J]. Journal of China Pharmaceutical University, 2023, 54(5): 564-568. DOI: 10.11665/j.issn.1000-5048.2023041002

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Synthesis and antifungal evaluation of chalcone derivatives combined with fluconazole against drug-resistant Candida albicans

School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, China

Funds: This study was supported by the Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Chinese Medicine [No.202001AZ070001-007, No.202101AZ070001-055, No.2019FF002 (029)]

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Received Date: April 09, 2023
Revised Date: October 16, 2023

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Abstract

Abstract

Chalcone is a common scaffold in natural products with optimal properties and biological activities.In this study, we designed and prepared eight new coumarin-chalcone derivatives (5a-5h), and confirmed their structures by ¹H NMR and ¹³C NMR. Their in vitro antifungal activity combined with fluconazole (FLC) against drug-resistant Candida albicans was tested by microdilution method.The results indicated that most chalcone derivatives showed good antifungal activity against drug resistant Candida albicans with FLC, particularly with compound 5g displaying better antifungal activity (MIC₅₀ = 5.60 μg/mL) than FLC (MIC₅₀ = 200 μg/mL) when combined with FLC, so, these derivatives could be used as synergists of antifungal drugs.
- chalcone derivatives,
- synthesis,
- antifungal activity,
- drug-resistant Candida albicans

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