Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 11, Pages 2585-2588Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.03.033
Keywords
Virtual screening; Fatty acid synthesis; Condensing enzymes; Antibiotics
Categories
Funding
- National Institutes of Health [5R01GM034496]
- Cancer Center Support [CA21765]
- American Lebanese Syrian Associated Charities (ALSAC)
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The elongation condensing enzymes in the bacterial fatty acid biosynthesis pathway represent desirable targets for the design of novel, broad-spectrum antimicrobial agents. A series of substituted benzoxazolinones was identified in this study as a novel class of elongation condensing enzyme (FabB and FabF) inhibitors using a two-step virtual screening approach. Structure activity relationships were developed around the benzoxazolinone scaffold showing that N-substituted benzoxazolinones were most active. The benzoxazolinone scaffold has high chemical tractability making this chemotype suitable for further development of bacterial fatty acid synthesis inhibitors. (C) 2014 Elsevier Ltd. All rights reserved.
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