Discovery of highly potent novel antifungal azoles by structure-based rational design

W Wang, C Sheng, X Che, H Ji, Y Cao, Z Miao…

Index: Wang, Wenya; Sheng, Chunquan; Che, Xiaoying; Ji, Haitao; Cao, Yongbing; Miao, Zhenyuan; Yao, Jianzhong; Zhang, Wannian Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 20 p. 5965 - 5969

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Citation Number: 29

Abstract

On the basis of the active site of lanosterol 14α-demethylase from Candida albicans (CACYP51), a series of new azoles were designed and synthesized. All the new azoles show excellent in vitro activity against most of the tested pathogenic fungi, which represent a class of promising leads for the development of novel antifungal agents. The MIC80 value of compounds 8c, 8i and 8n against C. albicans is 0.001 μg/mL, indicating that these ...