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Synthesis and biological evaluation of reversible inhibitors of IdeS, a bacterial cysteine protease and virulence determinant

På svenska

Author

  • Kristina Berggren
  • Björn Johansson
  • Tomas Fex
  • Jan Kihlberg
  • Lars Björck
  • Kristina Luthman

Summary, in English

Analogues of the irreversible protease inhibitors TPCK and TLCK have been synthesized and tested as inhibitors of the bacterial cysteine protease IdeS excreted by Streptococcus pyogenes. Eight compounds were identified as inhibitors of IdeS in an in vitro assay. The most potent compounds contained an aldehyde function, thus acting as efficient reversible inhibitors, nitrile and azide derivatives showed moderate activity. (C) 2009 Elsevier Ltd. All rights reserved.

Publishing year

2009

Language

English

Pages

3463-3470

Publication/Series

Bioorganic & Medicinal Chemistry

Volume

17

Issue

9

Document type

Journal article

Publisher

Elsevier

Topic

  • Infectious Medicine

Keywords

  • IdeS
  • Cysteine proteases
  • Reversible inhibitors
  • Streptococcus pyogenes

Status

Published

ISBN/ISSN/Other

  • ISSN: 0968-0896