Imidazole analogues of fluoxetine have been obtained by replacing the methylamino terminus of aminopropane chain with the imidazole ring. The newly designed imidazoles showed potent anti-Candida activity, superior to those of miconazole and other antifungal agents of clinical interest. 1-(4-Chlorophenyl)-1-(2,4-dichlorophenoxy)-3-(1H-imidazol-1-yl)propane (16), the most active among test imidazoles, was about 2-fold more active and as much less cytotoxic than miconazole. High increase of activity was observed with methyl, nitro, fluorine, and chlorine (Cl > F > CH(3) > NO(2) > CF(3)).
Imidazole Analogues of Fluoxetine, a Novel Class of Anti-Candida Agents / Silvestri, Romano; Artico, Marino; LA REGINA, Giuseppe; A., Di Pasquali; G., De Martino; D'Auria, Felicia Diodata; Nencioni, Lucia; Palamara, ANNA TERESA. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 47:(2004), pp. 3924-3926. [10.1021/jm049856v]
Imidazole Analogues of Fluoxetine, a Novel Class of Anti-Candida Agents.
SILVESTRI, Romano;ARTICO, Marino;LA REGINA, GIUSEPPE;D'AURIA, Felicia Diodata;NENCIONI, Lucia;PALAMARA, ANNA TERESA
2004
Abstract
Imidazole analogues of fluoxetine have been obtained by replacing the methylamino terminus of aminopropane chain with the imidazole ring. The newly designed imidazoles showed potent anti-Candida activity, superior to those of miconazole and other antifungal agents of clinical interest. 1-(4-Chlorophenyl)-1-(2,4-dichlorophenoxy)-3-(1H-imidazol-1-yl)propane (16), the most active among test imidazoles, was about 2-fold more active and as much less cytotoxic than miconazole. High increase of activity was observed with methyl, nitro, fluorine, and chlorine (Cl > F > CH(3) > NO(2) > CF(3)).I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
