2. Academic Validation
  3. Imidazole analogues of fluoxetine, a novel class of anti-Candida agents

Imidazole analogues of fluoxetine, a novel class of anti-Candida agents

  • J Med Chem. 2004 Jul 29;47(16):3924-6. doi: 10.1021/jm049856v.
Romano Silvestri 1,  Marino Artico,  Giuseppe La Regina,  Alessandra Di Pasquali,  Gabriella De Martino,  Felicia Diodata D'Auria,  Lucia Nencioni,  Anna Teresa Palamara
Affiliations

Affiliation

  • 1 Istituto Pasteur - Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Università degli Studi di Roma La Sapienza, P.le A. Moro 5, I-00185 Roma, Italy. [email protected]
PMID: 15267229 DOI: 10.1021/jm049856v
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)).

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