Antifungal evaluation of quinoline-chalcone derivatives combined with FLC against drug-resistant Candida albicans. (15th April 2023)

• Record Type: Journal Article
• Authors: Chai, Nannan; Sun, Aimei; Zhu, Xianhu; Li, Yanping; Wang, Ruirui; Zhang, Yi; Mao, Zewei
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 86(2023)
• Publication Date: 2023-04-15
• Subjects: Quinoline-chalcone -- Antifungal activity -- Drug-resistant Candida albicans -- Mechanistic study; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2023.129242
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: With the widespread clinical use of FLC, the FLC-resistant C. albicans greatly increases the difficulty of treatment, and drug combination becomes an important method to treat C. albicans infection. In this work, we have prepared a series of quinoline-chalcone derivatives in good yields, and in vitro antifungal activity against C. albicans were evaluated. The results indicated that most title compounds combined with FLC showed good antifungal activity against drug-resistant C. albicans. Further mechanism researches demonstrated that 6a and 6c combined with FLC could significantly inhibited growth and biofilm formation of C. albicans, induce ROS accumulation, impair the mitochondrial membrane, and decrease intracellular ATP concentrations.