Design and synthesis of cyclo[-Arg-Gly-Asp-Ψ(triazole)-Gly-Xaa-] peptide analogues by click chemistry

A simple and mild synthesis of a new family of cyclopeptide analogues cyclo[-Arg-Gly-Asp-Ψ(triazole)-Gly-Xaa-] that is obtained by cyclization with click chemistry was investigated. In addition, the method was also successfully expanded to the synthesis of their analogues of different ring sizes. The result supports the potential utility of click chemistry in the preparation of novel integrin domain-binding antagonists and other cyclopeptide analogues.