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A series of S-alkyl substituted thioglycolurils was prepared through the alkylation of corresponding thioglycolurils with halogenoalkanes and tested for their fungicidal activity against six phytopathogenic fungi from different taxonomic classes: Venturia inaequalis, Rhizoctonia solani, Fusarium oxysporum, Fusarium moniliforme, Bipolaris sorokiniana, and Sclerotinia sclerotiorum, and two pathogenic yeasts: Candida albicans and Cryptococcus neoformans var. grubii. A number of S-alkyl substituted thioglycolurils exhibited high activity against Venturia inaequalis and Rhizoctonia solani (85–100% mycelium growth inhibition), and moderate activity against other phytopathogens. S-Ethyl substituted thioglycolurils possessed a high activity against Candida albicans. Additionally, the hemolytic and cytotoxic properties of promising derivatives were determined using human red blood cells and human embryonic kidney cells, respectively. Two S-ethyl derivatives possessed both low cytotoxicity against normal human cells and high fungicidal activity against Candida albicans.

A number of substituted 2,2‐dimethyl‐6‐arylidene‐1‐triazol‐1‐ylmethylcyclohexanols and 2,2‐dimethyl‐6‐arylidene‐1‐imidazol‐1‐ylmethylcyclohexanols were prepared from 2‐methylcyclohexanone in four steps: Claisen–Schmidt condensation with substituted benzaldehydes, methylation of the resulting 2‐methyl‐6‐benzylidenecyclohexanones, conversion to the oxiranes by interaction with dimethylsulfonium methylide and reaction of the oxiranes with triazole or imidazole. The compounds obtained were tested for antifungal activity against five phytopathogenic fungi of different taxonomic classes. EC50 values were determined for all compounds. Structure–activity relationships are discussed in broad terms. Some of triazolymethyl‐substituted cyclohexanols obtained are more active than triadimenol. © 1997 SCI.