| Literature DB >> 18529046 |
Giuseppe La Regina1, Felicia Diodata D'Auria, Andrea Tafi, Francesco Piscitelli, Stefania Olla, Fabiana Caporuscio, Lucia Nencioni, Roberto Cirilli, Francesco La Torre, Nadja Rodrigues De Melo, Steven L Kelly, David C Lamb, Marino Artico, Maurizio Botta, Anna Teresa Palamara, Romano Silvestri.
Abstract
New 1-[(3-aryloxy-3-aryl)propyl]-1 H-imidazoles were synthesized and evaluated against Candida albicans and dermatophytes in order to develop structure-activity relationships (SARs). Against C. albicans the new imidazoles showed minimal inhibitory concentrations (MICs) comparable to those of ketoconazole, miconazole, and econazole, and were more potent than fluconazole. Several derivatives ( 10, 12, 14, 18- 20, 24, 28, 29, 30, and 34) turned out to be potent inhibitors of C. albicans strains resistant to fluconazole, with MIC values less than 10 microg/mL. Against dermatophytes strains, compounds 20, 25, and 33 (MIC <or= 5 microg/mL) were equipotent to ketoconazole, econazole, and miconazole. SARs of imidazoles 10- 44 were rationalized with reasonable accuracy by a previously developed quantitative pharmacophore for antifungal agents.Entities:
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Year: 2008 PMID： 18529046 DOI： 10.1021/jm800009r
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446