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Bioorg Med Chem Lett. 2009 Jul 15;19(14):3787-90. doi: 10.1016/j.bmcl.2009.04.034. Epub 2009 Apr 18.

Synthesis and biological evaluation of penem inhibitors of bacterial signal peptidase.

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1
Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.

Abstract

We report the first synthesis of a 5S penem, known to bind bacterial type I signal peptidase, from the commercially available and inexpensive 6-aminopenicillanic acid. We report the first in vivo activity of the compound and use structure-activity relationship studies to begin to define the determinants of signal peptidase binding and also to begin to optimize the penem as an antibiotic.

PMID:
19427205
DOI:
10.1016/j.bmcl.2009.04.034
[Indexed for MEDLINE]
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