Abstract
In a context of growing resistance to classical antifungal therapy, the design of new drugs targeting alternative pathways is highly expected. Benzofuro[3,2-d]pyrimidine derivatives, derived from (-)-cercosporamide, were synthesized and evaluated as potential Candida albicans PKC inhibitors in the aim of restoring susceptibility to azole treatment. Co-administration assay of benzofuropyrimidinedione 23 and fluconazole highlighted a synergistic effect on inhibition of cell growth of a Candida albicans resistant strain.
Keywords:
Antifungal activity; Benzofuro[3,2-d]pyrimidine; Candida albicans Pkc1; Cercosporamide; Fluconazole susceptibility restoration.
Copyright © 2018 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antifungal Agents / chemical synthesis
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Antifungal Agents / pharmacology*
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Ascomycota / chemistry
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Benzofurans / chemical synthesis
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Benzofurans / pharmacology*
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Biofilms / drug effects
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Candida albicans / drug effects
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Candida albicans / enzymology
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Drug Resistance, Fungal / drug effects*
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Drug Synergism
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Fluconazole / chemical synthesis
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Fluconazole / pharmacology
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HeLa Cells
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Humans
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Protein Kinase C / antagonists & inhibitors*
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / pharmacology*
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Pyrimidinones / chemical synthesis
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Pyrimidinones / pharmacology*
Substances
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Antifungal Agents
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Benzofurans
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Protein Kinase Inhibitors
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Pyrimidinones
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cercosporamide
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Fluconazole
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Protein Kinase C