Discovery of a novel broad-spectrum antifungal agent derived from albaconazole

ACS Med Chem Lett. 2013 Jan 17;4(2):288-92. doi: 10.1021/ml300429p. eCollection 2013 Feb 14.

Abstract

Synthesis of a strict structural analogue of albaconazole in which the quinazolinone ring is fused by a thiazole moiety led to the discovery of a new triazole with broad-spectrum antifungal activity. Compound I exhibited high in vitro activity against pathogenic Candida species and filamentous fungi and showed preliminary in vivo antifungal efficacy in a mice model of systemic candidiasis.

Keywords: Aspergillus; Candida; antifungal agents; azoles; thiazolo[4,5-g]quinazolin-8(7H)-one; zygomycetes.