Synthesis and biological evaluation of oxytocin analogues containing l-α-t-butylglycine [Gly(But)] in positions 8 or 9

Add time:09/02/2019    Source:sciencedirect.com

We report the solid phase synthesis and some pharmacological properties of seventeen new oxytocin (OT) analogues. Basic modification at positions 8 and/or 9 (introduction of l-α-t-butylglycine [Gly(But)]) was combined with d-Cys6, d-Tyr(Et)2, Mpa1 or Pen1 modifications and their various combinations. We also present properties of two previously reported re-synthesized analogues ([Gly(But)8]OT and [Mpa1, Gly(But)8]OT). The analogues were tested for rat uterotonic activity in vitro, in the rat pressor assay and for binding affinity to human OTR.

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