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. © The Royal Society of Chemistry.
CITATION STYLE
Bock, V. D., Speijer, D., Hiemstra, H., & Van Maarseveen, J. H. (2007). 1,2,3-Triazoles as peptide bond isosteres: Synthesis and biological evaluation of cyclotetrapeptide mimics. Organic and Biomolecular Chemistry, 5(6), 971–975. https://doi.org/10.1039/b616751a
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