1,2,3-Triazoles as peptide bond isosteres: synthesis and biological evaluation of cyclotetrapeptide mimics.

نویسندگان

  • Victoria D Bock
  • Dave Speijer
  • Henk Hiemstra
  • Jan H van Maarseveen
چکیده

Since the discovery of Cu(I)-catalysed click chemistry, the field of peptidomimetics has expanded to include 1,4-connected 1,2,3-triazoles as useful peptide bond isosteres. Here, we report the synthesis of triazole-containing analogues of the naturally occurring tyrosinase inhibitor cyclo-[Pro-Val-Pro-Tyr] and show that the analogues retain enzyme inhibitory activity, demonstrating the effectiveness of a 1,4-connected 1,2,3-triazole as a trans peptide bond isostere.

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عنوان ژورنال:
  • Organic & biomolecular chemistry

دوره 5 6  شماره 

صفحات  -

تاریخ انتشار 2007