Benzofuro[3, 2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration. Issue 13 (15th July 2018)

• Record Type: Journal Article
• Authors: Dao, Viet Hung; Ourliac-Garnier, Isabelle; Bazin, Marc-Antoine; Jacquot, Catherine; Baratte, Blandine; Ruchaud, Sandrine; Bach, Stéphane; Grovel, Olivier; Le Pape, Patrice; Marchand, Pascal
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 13(2018)
• Page Start: 2250
• Page End: 2255
• Publication Date: 2018-07-15
• Subjects: Cercosporamide -- Benzofuro[3, 2-d]pyrimidine -- Antifungal activity -- Candida albicans Pkc1 -- Fluconazole susceptibility restoration; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.05.044
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: Heterocyclic compounds inspired from cercosporamide were synthesized. Synergistic effect with fluconazole on inhibition of cell growth of a Candida albicans resistant strain is reported. Kinase inhibitory activity was detected. 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.