Get access

Maintaining Biological Activity by Using Triazoles as Disufide Bond Mimetics

Authors

  • Dr. Kai Holland-Nell,

    1. Leibniz-Insitut für Molekulare Pharmakologie, Robert-Rössle-Str. 10, 13125 Berlin (Germany)
    Search for more papers by this author
  • Prof. Morten Meldal

    Corresponding author
    1. Carlsberg Laboratory, Gamle Carlsberg Vej 10, 2500 Valby (Denmark), Fax: (+45) 3327-4708
    • Carlsberg Laboratory, Gamle Carlsberg Vej 10, 2500 Valby (Denmark), Fax: (+45) 3327-4708
    Search for more papers by this author

  • We would like to acknowledge the inspiring discussions and support from Prof. A. Beck-Sickinger and B. Petersen, and financial support by a PostDoc grant from the Deutsche Forschungsgemeinschaft.

Abstract

original image

Click into place: Tachyplesin-I (TP-I) analogues in which both disulfide bridges (1) have been replaced with triazoles (2) represent structural mimetics of TP-I that display similar or slightly improved antibacterial activity. Optimized structures were obtained by replacing the cysteine residues in TP-I by azido- and alkyno-functionalized amino acids.

Ancillary