Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives.
Eur J Med Chem
; 49: 334-42, 2012 Mar.
Article
en En
| MEDLINE
| ID: mdl-22321993
ABSTRACT
A new series of aromatic ester and carbamate derivatives of 2-(1H-imidazol-1-yl)-1-phenylethanol were synthesized and evaluated for their antifungal activity towards Candida albicans and non-albicans Candida species strains. The aromatic biphenyl ester derivatives 6a-c were more active than the reference compound fluconazole. 6c possesses a MIC mean values of 1.7 ± 1.4 µg mL(-1)vs C. albicans and 1.9 ± 2.0 µg mL(-1)vs non-albicans Candida species strains. The racemic mixtures of 6a, b were purified to afford the pure enantiomers. The (-) isomers were up to 500 times more active than (+) isomers. (-)-6a and (-)-6b were thirty and ninety times more active than fluconazole towards C. krusei strain respectively. The racemates of 6a-c showed low cytotoxicity against human monocytic cell line (U937) with 6a demonstrating a CC(50) greater than 128 µg mL(-1).
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Alcohol Feniletílico
/
Candida
/
Antifúngicos
Límite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Año:
2012
Tipo del documento:
Article
País de afiliación:
Italia