THE SYNTHESIS OF AMINIMIDE-CONTAINING AZOLE ANTIFUNGALS

The synthesis of a series of azole antifungal compounds which incorpor ate the aminimide functional moiety is described. The procedure involv es the reaction of an epoxide intermediate with 1,1-disubstituted hydr azines to form aminimines which are subsequently treated with acyl chl orides resulting in the desired zwitterionic aminimides. The aminimide s were tested for in vitro antifungal activity and found to be moderat ely active against Candida and Cryptococcus species, but inactive vers us Aspergillus.