A new class of antifungal agents. Synthesis and antimycotic activity of disubstituted N-azolylamines

In this study we extended our exploration of the N-azolylamine moiety for i ts antifungal activity. We prepared a number of N-azolylamino derivatives. The synthetic sequence includes the preparation of aminoazole Schiff bases, and the reduction and the alkylation of the corresponding secondary amines . The title compounds were evaluated in vitro against several pathogenic fu ngi responsible for human disease. The most potent antimicrobial compound w as the N-(biphenyl-4-yl)methyl-N-(2,4-dichlorophenyl)methyl-1H-imidazol-1-y lamine (21), which was found to be active against yeasts and dermatophytes; its potency and selectivity were comparable to those of miconazole.