Synthesis and antifungal activity of (Z)-5-arylidenerhodanines
- Sortino, Maximiliano Andrés
- Delgado, Paula
- Juárez, Sabina
- Quiroga, Jairo
- Abonía, Rodrigo
- Insuasty, Braulio
- Nogueras, Manuel
- Rodero, Laura
- Garibotto, Francisco Matías
- Enriz, Ricardo Daniel
- Zacchino, Susana Alicia Stella
DOIAbstract
An efficient microwave-assisted synthesis of new (Z)-5-arylidenerhodanines under solvent-free conditions is described and their in vitro antifungal activity was evaluated following the CLSI (formerly NCCLS) guidelines against a panel of both standardized and clinical opportunistic pathogenic fungi. An analysis of the structure-activity relationship (SAR) along with computational studies showed that the most active compounds (F- and CF3-substituted rhodanines) possess high log P values and low polarizability. Mechanism-based assays suggest that active compounds neither would bind to ergosterol nor would produce a damage to the fungal membrane.Fil: Sortino, Maximiliano Andrés. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas ...
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