Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration |
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| Authors: | Viet Hung Dao Isabelle Ourliac-Garnier Marc-Antoine Bazin Catherine Jacquot Blandine Baratte Sandrine Ruchaud Stéphane Bach Olivier Grovel Patrice Le Pape Pascal Marchand |
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| Affiliation: | 1. Université de Nantes, Nantes Atlantique Universités, Département de Chimie Thérapeutique, EA1155 – IICiMed, Institut de Recherche en Santé 2, F-44200 Nantes, France;2. Université de Nantes, Nantes Atlantique Universités, Département de Parasitologie et Mycologie Médicale, EA1155 – IICiMed, Institut de Recherche en Santé 2, F-44200 Nantes, France;3. Sorbonne Université, CNRS, Plateforme de criblage KISSf (Kinase Inhibitor Specialized Screening facility), USR Protein Phosphorylation and Human Diseases, Station Biologique, Place Georges Teissier, F-29688 Roscoff, France;4. Université de Nantes, Nantes Atlantique Universités, EA2160 – Mer Molécules Santé, Faculté de Pharmacie, F 44035 Nantes, France |
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| 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. |
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| Keywords: | Cercosporamide Antifungal activity Fluconazole susceptibility restoration |
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