Design and Synthesis of 24-Fluorinated Bafilomycin Analogue as an NMR Probe with Potent Inhibitory Activity to Vacuolar-type ATPase

被引：4

作者：

Shibata, Hajime ^{[1
,2
]}

Tsuchikawa, Hiroshi ^{[1
]}

Matsumori, Nobuaki ^{[1
]}

Murata, Michio ^{[1
,2
]}

Usui, Takeo ^{[3
]}

机构：

[1] Osaka Univ, Grad Sch Sci, Toyonaka, Osaka 5600043, Japan

[2] Japan Sci & Technol Agcy, Lipid Act Struct Project, ERATO, Toyonaka, Osaka 5600043, Japan

[3] Univ Tsukuba, Fac Life & Environm Sci, Tsukuba, Ibaraki 3058572, Japan

来源：

CHEMISTRY LETTERS | 2014年 / 43卷 / 04期

关键词：

SOLID-STATE NMR; MACROLIDE ANTIBIOTICS; AMPHOTERICIN-B; H+-ATPASE; A(1); MEMBRANE; F-19; MICROORGANISMS; DERIVATIVES; PHYSIOLOGY;

D O I：

10.1246/cl.131099

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A fluorine-labeled bafilomycin analogue was designed and convergently synthesized from three segments via the Stille coupling, macrolactonization, and diastereoselective aldol reaction. The V-ATPase inhibitory activity of the analogue was comparable to that of the natural product, indicating its utility as a potential molecular probe for investigating the inhibition mechanism of bafilomycin by NMR.

引用

页码：474 / 476

页数：3

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