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ID: ALA4118230

Journal: Bioorg Med Chem Lett

Title: Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration.

Authors: Dao VH, Ourliac-Garnier I, Bazin MA, Jacquot C, Baratte B, Ruchaud S, Bach S, Grovel O, Le Pape P, Marchand P.

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.

CiteXplore: 29853332

DOI: 10.1016/j.bmcl.2018.05.044