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Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: Synthesis and evaluation of fluconazole susceptibility restoration
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-05-23 , DOI: 10.1016/j.bmcl.2018.05.044
Viet Hung Dao , Isabelle Ourliac-Garnier , Marc-Antoine Bazin , Catherine Jacquot , Blandine Baratte , Sandrine Ruchaud , Stéphane Bach , Olivier Grovel , Patrice Le Pape , Pascal Marchand

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.



中文翻译:

cercosporamide Ca Pkc1抑制剂激发的苯并呋喃[3,2- d ]嘧啶类药物:氟康唑敏感性恢复的合成和评价

在对经典抗真菌疗法的抗药性日益增长的背景下,人们迫切希望设计出靶向替代途径的新药。合成了源自(-)-cercosporamide的Benzofuro [3,2- d ]嘧啶衍生物,并作为潜在的白色念珠菌PKC抑制剂进行了评估,目的是恢复对唑处理的敏感性。苯并呋喃基嘧啶二酮23和氟康唑的共同给药分析突出显示了对白色念珠菌抗性菌株的细胞生长抑制的协同作用。

更新日期:2018-05-23
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