(±) cis-bisamido epoxides: A novel series of potent FXIII-A inhibitors

Craig A. Avery, Richard J. Pease, Kerrie Smith, May Boothby, Helen M. Buckley, Peter J. Grant, Colin W.G. Fishwick

Research output: Contribution to journalArticlepeer-review

10 Citations (Scopus)


A novel class of potent FXIII-A inhibitors containing a (±) cis-bisamido epoxide pharmacophore is described. The compounds display highly potent inhibition of FXIII-A (IC50 Combining double low line 5-500 nM) in an in vitro assay. In contrast to other types of previously described covalent transglutaminase inhibitors, the bis-Amido epoxides exhibited no measurable reactivity with glutathione, therefore possibly rendering this class of compounds suitable for future in vivo investigations. Additionally, the compounds show selective inhibition for FXIII-A against the cysteine protease, cathepsin S although they proved to have similar potency with a closely related transglutaminase, TGII, to that observed for FXIII-A.

Original languageEnglish
Pages (from-to)49-53
Number of pages5
JournalEuropean Journal of Medicinal Chemistry
Publication statusPublished - 26 May 2015
Externally publishedYes


  • Bis-Amido epoxides molecular modelling
  • Thrombosis


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