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Bioorg Med Chem Lett. 2010 Oct 15;20(20):6116-20. doi: 10.1016/j.bmcl.2010.08.037. Epub 2010 Aug 18.

Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.

Author information

1
Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, Tokyo, Japan.

Abstract

Novel bottromycin derivatives were synthesized from bottromycin A(2) via a hydrazide derivative as a common intermediate. Seventeen derivatives were subjected to in vitro evaluation against drug-resistant gram-positive bacteria. Some compounds showed potent anti-MRSA and anti-VRE activity, as did bottromycin A(2). Notably, a propyl ketone derivative exhibited good antibacterial activity with excellent metabolite stability.

PMID:
20833545
DOI:
10.1016/j.bmcl.2010.08.037
[Indexed for MEDLINE]

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