期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 14, 页码 3787-3790出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.034
关键词
Antibiotic; SAR; Staphylococcus epidermidis; MRSA
资金
- Office of Naval Research [N00014-08-1-0478, N00014-03-1-0126]
- Achaogen Inc.
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. (C) 2009 Elsevier Ltd. All rights reserved.
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