Tentoxin as a Scaffold for Drug Discovery. Total Solid-Phase Synthesis of Tentoxin and a Library of Analogues

A solid-phase method for the synthesis of tentoxin has been developed. Two key stepsdehydration and N-alkylationare carried out while the peptide is anchored to the resin. The method, which has been validated by the preparation of a library of tentoxin analogues, should be applicable to the generation of further libraries that have the tentoxin scaffold structure, as well as other structures containing N-alkylated didehydroamino acids.