Fluconazole-COX Inhibitor Hybrids: A Dual-Acting Class of Antifungal Azoles
Rebecca Elias, Pallabita Basu, Micha Fridman
Abstract
-configured pharmacophore. Tolerance, defined as the ability of a subpopulation of cells to grow in the presence of the drug, to the hybrids was lower than to fluconazole and voriconazole. The hybrids were active against a mutant lacking CYP51, the target of azole drugs, indicating that these agents act via a dual mode of action. This study established that azole-COX inhibitor hybrids are a novel class of potent antifungals with clinical potential.
Topics & Concepts
AzolePharmacophoreFluconazoleChemistryVoriconazolePharmacologyCryptococcus neoformansAntifungalMicrobiologyBiochemistryBiologyAntifungal resistance and susceptibilitySynthesis and Biological EvaluationInflammatory mediators and NSAID effects