Synthesis of potent water-soluble tissue transglutaminase inhibitors

Martin Griffin, Alexandre Mongeot, Russell Collighan, Robert E. Saint, Richard A. Jones, Ian G.C. Coutts, Daniel L. Rathbone

Research output: Contribution to journalArticle

Abstract

Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.
LanguageEnglish
Pages5559-5562
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number20
DOIs
Publication statusPublished - 15 Oct 2008

Fingerprint

Diazooxonorleucine
Lead compounds
Transglutaminases
Dipeptides
Water
transglutaminase 2
Lead

Keywords

  • transglutaminase
  • inhibitors
  • dipeptide

Cite this

Griffin, Martin ; Mongeot, Alexandre ; Collighan, Russell ; Saint, Robert E. ; Jones, Richard A. ; Coutts, Ian G.C. ; Rathbone, Daniel L. / Synthesis of potent water-soluble tissue transglutaminase inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2008 ; Vol. 18, No. 20. pp. 5559-5562.
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Synthesis of potent water-soluble tissue transglutaminase inhibitors. / Griffin, Martin; Mongeot, Alexandre; Collighan, Russell; Saint, Robert E.; Jones, Richard A.; Coutts, Ian G.C.; Rathbone, Daniel L.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 18, No. 20, 15.10.2008, p. 5559-5562.

Research output: Contribution to journalArticle

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