Novel 2-aminotetralin compounds were designed and synthesized based on the three-dimensional model of lanosterol 14α-demethylase of Candida albicans. Their structures have been confirmed by ¹H NMR, IR and MS. All these compounds, especially compounds 18, 21, 22 and 24 exhibited potent antifungal activities against seven pathogenic fungi. The mode of the action of the lead compound was different from that of azoles, and the lead compound interacted with the amino acid residues in the active site. These aminotetralins provided lead compounds for the development of antifungal drugs.

Key words: antifungal, 2-aminotetralin, lanosterol 14α-demethylase inhibitor