Synthesis and antifungal activities of (2R, 3R)-2-aryl-1-azolyl-3-(substituted amino)-2-butanol derivatives as topical antifungal agents

Many kinds of topical antifungal agents have been developed and are available as commercial products. These agents are classified into a number of groups, i.e. allylamines, benzylamines, imidazoles, thiocarbamates and morpholines, which exhibit quite different biological properties. Benzylamines and allylamines show strong antifungal activities against dermatophytes such as Trichophyton mentagrophytes, but show weak activity against yeast-like fungi such as Candida albicans. Thiocarbamates and morpholines show very weak effects against yeast-like fungi and Aspergillus spp., respectively. Imidazoles have moderate antifungal activities, but their activity and spectra are wider than those of the other groups. These agents are used for the treatment of dermatomycosis, but relapse of infection is often observed after therapy. Therefore, there it is still necessary to develop new topical antifungal agents with broad spectrum, strong in vitro antifungal activity and excellent therapeutic efficacy.