1. Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.
- Author
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Dao VH, Ourliac-Garnier I, Bazin MA, Jacquot C, Baratte B, Ruchaud S, Bach S, Grovel O, Le Pape P, and Marchand P
- Subjects
- Antifungal Agents chemical synthesis, Ascomycota chemistry, Benzofurans chemical synthesis, Biofilms drug effects, Candida albicans drug effects, Candida albicans enzymology, Drug Synergism, Fluconazole chemical synthesis, Fluconazole pharmacology, HeLa Cells, Humans, Protein Kinase Inhibitors chemical synthesis, Pyrimidinones chemical synthesis, Antifungal Agents pharmacology, Benzofurans pharmacology, Drug Resistance, Fungal drug effects, Protein Kinase C antagonists & inhibitors, Protein Kinase Inhibitors pharmacology, Pyrimidinones pharmacology
- 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., (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Published
- 2018
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