The de novo design of peptides and proteins represents an innovative tool in the early stage
of drug research. Over the last thirty years, many studies have been undertaken to develop new
strategies of design and synthesis of peptides with specific conformations. Substituted amino acids
exhibit significant biological activity, and play an important role in medicinal chemistry. Proline
chimeras in particular, are valuable tools for biological investigations. In the literature several
strategies for the synthesis of this chimeras are reported. Here we will focus on Tryptophan-Proline
and summarize useful methodologies that can be applied to their preparation.
Keywords: Tryptophan-Proline chimeras, substituted proline, peptide, synthesis.
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