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

Research output: Contribution to journalArticle

Abstract

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.

Details

Authors
  • Kristina Berggren
  • Björn Johansson
  • Tomas Fex
  • Jan Kihlberg
  • Lars Björck
  • Kristina Luthman
Organisations
Research areas and keywords

Subject classification (UKÄ) – MANDATORY

  • Infectious Medicine

Keywords

  • IdeS, Cysteine proteases, Reversible inhibitors, Streptococcus pyogenes
Original languageEnglish
Pages (from-to)3463-3470
JournalBioorganic & Medicinal Chemistry
Volume17
Issue number9
Publication statusPublished - 2009
Publication categoryResearch
Peer-reviewedYes