Synthesis and antifungal activity of polycyclic pyridone derivatives with anti-hyphal and biofilm formation activity against Candida albicans

[Display omitted] 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...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2021-04, Vol.37, p.127845-127845, Article 127845
Main Authors: Kamauchi, Hitoshi, Kimura, Yu, Ushiwatari, Mikoto, Suzuki, Mitsuaki, Seki, Taishi, Takao, Koichi, Sugita, Yoshiaki
Format: Article
Language:English
Subjects:
Biofilm formation
Candida albicans
Hyphal formation
Pyridone
XTT reduction assay
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] 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 anti-hyphal and biofilm inhibition activity.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2021.127845