Quaternised nitrogen-containing azole antifungals

Abstract

The application claims a series of synthetic imidazole or triazole compounds in which one of the nitrogen atoms in the azole ring is quaternised with a substituent capable of being eliminated in vivo, resulting in an active antifungal azole compound. The application contains a total of 42 claims describing analogues, formulations and processes. The application intends treatment of fungal infections in mammals as the primary use of the compounds but also indicates their suitability as agricultural fungicides. The methods of administration are broad, including oral, parenteral and topical routes, and a number of possible formulations are described. Select compounds were evaluated in a mouse model of systemic candidiasis, with activity demonstrated by both the oral and iv. routes of administration.

• antifungal
• azole
• imidazole
• quaternary nitrogen
• synthetic
• triazole