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

Author

Takayuki Tonoi, Takehiko Inohana, Teruyuki Sato, Yuuki Noda, Miyuki Ikeda, Miku Akutsu, Takatsugu Murata, Yutaro Maekawa, Anna Tanaka, Rio Seki, Misako Ohkusu, Katsuhiko Kamei, Naruhiko Ishiwada, and Isamu Shiina

Subjects
eushearilide, demethyl congener, total synthesis, lactonization, MNBA, antimicrobial activity, Organic chemistry, QD241-441
Abstract

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).

Published
2019
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