Literature DB >> 17869508

Design and synthesis via click chemistry of 8,9-anhydroerythromycin A 6,9-hemiketal analogues with anti-MRSA and -VRE activity.

Akihiro Sugawara1, Toshiaki Sunazuka, Tomoyasu Hirose, Kenichiro Nagai, Yukie Yamaguchi, Hideaki Hanaki, K Barry Sharpless, Satoshi Omura.   

Abstract

An erythromycin analogue, 11,12-di-O-iso-butyryl-8,9-anhydroerythromycin A 6,9-hemiketal (1b), was found to be a potential anti-MRSA and anti-VRE agent. The use of copper catalyzed azide-acetylene cycloaddition, and click chemistry, readily provided 10 types of triazole analogues of 1b in good to nearly quantitative yield. Among the library, 5b exhibited activity against MRSA and VRE bacterial strains, representing more than twice the potency of 1b.

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Year:  2007        PMID: 17869508     DOI: 10.1016/j.bmcl.2007.08.068

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  5-O-Mycaminosyltylonolide antibacterial derivatives: design, synthesis and bioactivity.

Authors:  Akihiro Sugawara; Hitomi Maruyama; Sho Shibusawa; Hidehito Matsui; Tomoyasu Hirose; Ayumi Tsutsui; Robrecht Froyman; Carolin Ludwig; Johannes Koebberling; Hideaki Hanaki; Gerd Kleefeld; Satoshi Ōmura; Toshiaki Sunazuka
Journal:  J Antibiot (Tokyo)       Date:  2017-05-31       Impact factor: 2.649

  1 in total

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