Carboxylic acid and phosphate ester derivatives of fluconazole: synthesis and antifungal activities

NH Nam, S Sardari, M Selecky, K Parang

文献索引：Nam, Nguyen-Hai; Sardari, Soroush; Selecky, Meredith; Parang, Keykavous Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 23 p. 6255 - 6269

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被引用次数: 45

摘要

Two classes of fluconazole derivatives,(a) carboxylic acid esters and (b) fatty alcohol and carbohydrate phosphate esters, were synthesized and evaluated in vitro against Cryptococcus neoformans, Candida albicans, and Aspergillus niger. All carboxylic acid ester derivatives of fluconazole (1a–l), such as O-2-bromooctanoylfluconazole (1g, MIC= 111μg/mL) and O-11-bromoundecanoylfluconazole (1j, MIC= 198μg/mL), exhibited higher ...