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. 2018 Jul 15;28(13):2250-2255.
doi: 10.1016/j.bmcl.2018.05.044. Epub 2018 May 23.

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

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

Viet Hung Dao et al. Bioorg Med Chem Lett. .

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.

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