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

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.

• Författare: Kristina Berggren; Björn Johansson; Tomas Fex; Jan Kihlberg; Lars Björck; Kristina Luthman
• Avdelning/ar: Infektionsmedicin
• Publiceringsår: 2009
• Språk: Engelska
• Sidor: 3463-3470
• Publikation/Tidskrift/Serie: Bioorganic & Medicinal Chemistry
• Volym: 17
• Issue: 9
• Länkar: http://dx.doi.org/10.1016/j.bmc.2009.03.026
• Dokumenttyp: Artikel i tidskrift
• Förlag: Elsevier
• Ämne: Infectious Medicine
• Nyckelord: IdeS; Cysteine proteases; Reversible inhibitors; Streptococcus pyogenes
• Status: Published
• ISBN/ISSN/Övrigt: ISSN: 0968-0896