Details

Autor(en) / Beteiligte

• Bin YAO
• You Jun ZHOU
• Jü ZHU
• Jia Guo L(U)
• Yao Wu LI
• Jun CHENG
• Qing Feng JIANG
• Can Hui ZHENG

Titel

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

Ist Teil von

• 中国化学快报（英文版）, 2006-09, Vol.17 (9), p.1189-1192

Ort / Verlag

School of Pharmacy, Second Military Medicial University, Shanghai 200433

Erscheinungsjahr

2006

Beschreibungen/Notizen

• O6; 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.