The synthesis of aminimidecontaining azole antifungals

Autor: Abel, Mark D., Hewgill, Randy T., Malczyk, Katherine J., Micetich, Ronald G., Daneshtalab, Mohsen
Zdroj: Journal of Heterocyclic Chemistry; January 1998, Vol. 35 Issue: 1 p193-199, 7p
Abstrakt: 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 1,1disubstituted hydrazines to form aminimines which are subsequently treated with acyl chlorides resulting in the desired zwitterionic aminimides. The aminimides were tested for in vitroantifungal activity and found to be moderately active against Candidaand Cryptococcusspecies, but inactive versus Aspergillus.
Databáze: Supplemental Index