Abstract: Benzylamine and azole compounds respectively inhibit squelene exoxidase and cytochrome P450 monooxygenase which are two key enzymes in biosynthesis of fungal membrances. According to the structure-activitity relationships and antimycotic mechanism of azole and benzylamine compounds, we combined the feature of structure of those two kinds of compounds to design and synthesize twenty three 1-[2-(N-methyl-N-substituted-benzyl)amino-2-(4-tert-butylphenyl)ethyl] -1-H-1,2,4-triazoles. All of them were first reported and their structures were confirmed by elementary analysis, IRand ¹H NMRspectra. The results of preliminary antifungal tests in vitro showed that all the compounds were active against the nine pathogenic fungi to some degrees. The activities against shallow fungi are greater than those of the deep ones. Compounds 3, 4, 6, 10, 12, 14 and 15 exhibited potent activities against microsporum canis.

Key words: 1,2,4-Triazolyl benzylamines, Fungicidal activity, Synthesis, Structure-activity relationship