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Synthesis and biological evaluation of penem inhibitors of bacterial signal peptidase

Academic Article
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Overview

related to degree

  • Harris, David A, Ph.D. in Chemistry, Scripps Research 2004 - 2012

authors

  • Harris, David A
  • Powers, M. E.
  • Romesberg, Floyd

publication date

  • July 2009

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

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.

subject areas

  • Anti-Bacterial Agents
  • Membrane Proteins
  • Microbial Sensitivity Tests
  • Penicillanic Acid
  • Serine Endopeptidases
  • Serine Proteinase Inhibitors
  • Structure-Activity Relationship
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Research

keywords

  • Antibiotic
  • MRSA
  • SAR
  • Staphylococcus epidermidis
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2009.04.034

PubMed ID

  • 19427205
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Additional Document Info

start page

  • 3787

end page

  • 3790

volume

  • 19

issue

  • 14

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