Citation: Bin YAO, You Jun ZHOU, Jü ZHU, Jia Guo Lü, Yao Wu LI, Jun CHENG, Qing Feng JIANG, Can Hui ZHENG. Design, Synthesis and Biological Evaluation of Non-azole Inhibitors of Lanosterol 14α-Demethylase of Fungi[J]. Chinese Chemical Letters, ;2006, 17(9): 1189-1192. shu

Design, Synthesis and Biological Evaluation of Non-azole Inhibitors of Lanosterol 14α-Demethylase of Fungi

School of Pharmacy, Second Military Medicial University, Shanghai 200433

Received Date: 27 March 2006

Fund Project: The work was supported by the National Natural Science Foundation of China (No. 30572257).

Novel tetralin compounds were designed and synthesized on the three-dimensional model of lanosterol 14α-demethylase of Candida albicans. All of the lead compounds exhibited potent antifungal activities, especially compounds 16, 20. The mode of the action of the lead compounds was different from that of azoles. The present study affords the possibility to develop novel antifungal agents that specifically interact with the amino acid residues in the active site and avoid the serious toxicity arising from coordination binding with the heme of mammalian P450s.
- Antifungal,
- 2-aminotetralins,
- lanosterol 14α-demethylase,
- inhibitor
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