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


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.

SUBMITTER: Guillon R 

PROVIDER: S-EPMC4027234 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature

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

Guillon Rémi R   Pagniez Fabrice F   Picot Carine C   Hédou Damien D   Tonnerre Alain A   Chosson Elizabeth E   Duflos Muriel M   Besson Thierry T   Logé Cédric C   Le Pape Patrice P  

ACS medicinal chemistry letters 20130117 2


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. ...[more]

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