Solid-phase synthesis of olefin-containing HTLV-1 protease inhibitor using Horner-Emmons reaction

摘要

The introduction of an olefin structure into a peptide backbone is a promising approach for inducing conformational change,and thus is an important design consideration in peptidemimetics.Little information,however,is available concerning the construction of an olefin peptidemimetic on a solid support as well as the biological evaluations of olefin peptidemimetics.In this work,we applied the solid phase Horner-Emmons reaction for the introduction of an olefin bond into the substrate sequence of Human T-cell Leukemia virus type I(HTLV-1)protease,for which few inhibitors have been reported to date.