Antifungal Activity of 1-phenyl-5-benzylsulfanyltetrazoles

Jan Adamec¹, Karel Waisser¹ (waisser@faf.cuni.cz), Luís Silva², Vladimír Buchta²

¹ Department of Inorganic and Organic Chemistry, ² Department of Biological and Medical Sciences, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Czech Republic

Summary

The purpose of this study was to investigate the structure--antifungal activity relationships in the group of 19 compounds, derivatives of 1-phenyl-5-benzylsulfanyltetrazoles, in which phenyl in position 1 of tetrazole was substituted in position 4 by chlorine, methyl or methoxy group (or by chlorine in position 3 and 4), and by chlorine, methyl or methoxy group in position 4 of benzyl moiety. The goal of this paper was to study in vitro antifungal activity of antimycobacterial tetrazole against Candida albicans ATCC 44859, Candida tropicalis 156, Candida krusei E28, Candida glabrata 20/I, Trichosporon beigelii 1188, Trichophyton mentagrophytes 445, Aspergillus fumigatus 231, Absidia corymbifera 272. The activity against the eight fungal strains were negligible with the exception of T. mentagrophytes and A. fumigatus. The structure--activity relationships against T. mentagrophytes were determined using the Free-Wilson method, which was further combined with the approach of Hansch.