The synthesis of aminimide-containing azole antifungals

Article abstract of DOI:10.1002/jhet.5570350137

The synthesis of a series of azole antifungal compounds which incorporate the aminimide functional moiety is described. The procedure involves the reaction of an epoxide intermediate with 1,1-disubstituted hydrazines to form aminimines which are subsequently treated with acyl chlorides resulting in the desired switterionic aminimides. The aminimides were tested for in vitro antifungal activity and found to be moderately active against Candida and Cryptococcus species, but inactive versus Aspergillus.