Novel Synthetic Strategies for the Development of Tryptophan-Proline Chimeras, Useful Tool for Drug Discovery

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.