23-去甲基耳壳海绵内酯的全合成及抗菌活性评价以及(16,20)-耳壳海绵内酯和(16,20)-异耳壳海绵内酯所有合成立体异构体的广泛抗菌活性评价

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

作者信息

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

机构信息

Department of Applied Chemistry, Faculty of Science, Tokyo University of Science, 1-3 Kagurazaka, Shinjuku-ku, Tokyo 162-8601, Japan.

Department of Infectious Diseases, Medical Mycology Research Center, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba-shi, Chiba 260-8673, Japan.

出版信息

Molecules. 2019 Sep 22;24(19):3437. doi: 10.3390/molecules24193437.

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 (MRSA) and vancomycin-resistant enterococci (VRE).