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Synthesis and biological evaluation of new biphalin analogues with non-hydrazine linkers
Adriano Mollica1, Peg Davis, Shou-Wu Ma
1Department of Chemistry, University of Arizona, Tucson, Arizona 85721, USA.
Bioorganic & Medicinal Chemistry Letters
|May 3, 2005
Abstract:
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.
