4.6 Article

Total Synthesis and Antimicrobial Evaluation of 23-Demethyleushearilide and Extensive Antimicrobial Evaluation of All Synthetic Stereoisomers of (16Z,20E)-Eushearilide and (16E,20E)-Eushearilide

Journal

MOLECULES
Volume 24, Issue 19, Pages -

Publisher

MDPI
DOI: 10.3390/molecules24193437

Keywords

eushearilide; demethyl congener; total synthesis; lactonization; MNBA; antimicrobial activity

Funding

  1. Ministry of Education, Science, Sports, and Culture, Japan

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A novel stereoisomer of eushearilide, 23-demethyleushearilide, was synthesized, and the structure-activity relationships of this compound along with known eushearilide stereoisomers were investigated in order to design novel lead compounds for the treatment of fungal infections. It was discovered that all of these congeners, together with the natural product, exhibited a wide range of antimicrobial activity against not only fungi but also against bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE).

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