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The synthesis and evaluation of 6-alkylidene-2'β-substituted penam sulfones as β-lactamase inhibitors

Academic Article
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Overview

authors

  • Buynak, J. D.
  • Rao, A. S.
  • Doppalapudi, V. R.
  • Adam, Gregory
  • Petersen, P. J.
  • Nidamarthy, S. D.

publication date

  • July 1999

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • Penicillin sulfones, which structurally incorporate both a 6-position alkylidene substituent and a 2'beta substituent, have been synthesized and evaluated as inhibitors of class C and class A serine beta-lactamases. Incorporation of the 2'beta-substituent generally improves inhibitory activity. Substituents that improve transport across the bacterial cell membrane have also been incorporated.

subject areas

  • Cloxacillin
  • Drug Therapy, Combination
  • Enzyme Inhibitors
  • Inhibitory Concentration 50
  • Microbial Sensitivity Tests
  • Penicillin Resistance
  • Piperacillin
  • Structure-Activity Relationship
  • Sulfones
  • beta-Lactamase Inhibitors
  • beta-Lactamases
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/s0960-894x(99)00325-x

PubMed ID

  • 10450969
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Additional Document Info

start page

  • 1997

end page

  • 2002

volume

  • 9

issue

  • 14

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