Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers

Biphalin is a potent opioid peptide agonist, with a palandromic structure, composed of two enkephalin-like active fragments connected tail to tail by a hydrazine linker (Tyr-D-Ala-Gly-Phe-NH-NH<-Phe<-Gly<-D-Ala<-Tyr). This study presents the synthesis and in vitro bioassays of six new biphalin analogues with three different non-hydrazine linkers, some of which have higher binding affinity and bioactivity than biphalin.

Graphical abstractThis study presents the synthesis and in vitro bioassay of new biphalin analogues with three novel non-hydrazine linkers.Figure optionsDownload full-size imageDownload as PowerPoint slide