Synthesis and antifungal activity of polycyclic pyridone derivatives with anti-hyphal and biofilm formation activity against Candida albicans
Synthesis and antifungal activity of polycyclic pyridone derivatives with anti-hyphal and biofilm formation activity against Candida albicans
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DOI：
10.1016/j.bmcl.2021.127845
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发表时间：
2021-02-18
影响因子：
2.7
通讯作者：
Sugita, Yoshiaki
中科院分区：
文献类型：
--
作者：
Kamauchi, Hitoshi;Kimura, Yu;Sugita, Yoshiaki
通过Domino-Knoevenagel-电环化反应，以多环吡啶酮为骨架，包括顺式或反式氧十氢萘和其他环状结构，合成了35个吡啶酮衍生物。对所合成的化合物进行了抗白色念珠菌的活性测试。10个化合物抑制菌丝形成，而不抑制生长。测试具有抗菌丝形成活性的吡啶酮（4c、6d、12 a和12 c）抑制生物膜形成的能力。化合物6d具有抑菌活性和生物膜抑制活性。
Thirty-five pyridone derivatives were synthesized, with derivatization conducted on polycyclic pyridone scaffolds, including cis-or trans-oxydecalin and other cyclic structures, by domino-Knoevenagel-electrocyclic reactions. The anti-fungal activities of the synthesized compounds were tested against Candida albicans. Ten compounds inhibited hyphal formation without inhibiting growth. Pyridones with anti-hyphal formation activity (4c, 6d, 12a and 12c) were tested for their ability to inhibit biofilm formation. Compound 6d showed both antihyphal and biofilm inhibition activity.