Development of Antifungal Hypervalent Iodonium Salts

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A variety of alkenyl- and alkynyl (phenyl) iodonium tetrafluoroborates were prepared from organosilanes. The in vitro and in vivo antifungal activity of the iodonium salts were studied and compared with that of amphotericin B,5-fluorocytosine, clotrimazole, and ketoconazole. The following results were obtained :1) (E)-1-Decenyl (phenyl) iodonium, 3-cyclopentyl-2-methylpropenyl (phenyl)-iodonium, and 2-methyl-3-phenylpropenyl (phenyl) iodonium tetrafluoroborates showedthe weak in vitro antifungal activity.2) n-Octynyl-, n-nonynyl, and n-undecynyl (phenyl) iodonium tetrafluoroborates were found to have a broad in vitro antifungal activity at low drug concentrations, inhibiting growth of Candida albicans, Candida albicans, Candida kursei, Candida tropicalis, Cryptococcous neoformans, Cryptococcous neoformans, Aspergillus fumigatus, Microsporum canis, Trichophyton mentagrophytes, Trichophyton rubrum. The activity varied remarkably with the culture medium : in the yeast nitrogen base agar at ph 5.6 the antifungal activity was observed.3) These alkenyl- and alkynyl (phenyl) iodonium tetrafluoroborates showed no in vivo antifungal activity.