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Abstract

Template-fixed .beta.-hairpin loop mimetics comprising a template corresponding to one of the structures (a), (b), (c), (d), (e), (f), (g), (h) and a template-fixed chain of 4 to 20 .alpha.-amino acid residues which, if their .alpha.-C atom is asymmetric, have L-configuration can be manufactured by a novel process which is based on a mixed solid- and solution phase synthetic strategy. If desired, this process can be modified to give the enantiomers of these template-fixed .beta.-hairpin loop mimetics. These enantiomers are novel compounds, and many of said template-fixed .beta.-hairpin loop mimetics themselves are also novel compounds. The template-fixed .beta.-hairpin loop mimetics and their enantiomers can mimic flat surfaces of proteins and thus be used to probe large surface protein-protein interactions. Accordingly they can serve as lead finding tools for protein targets where it is difficult to find small-molecular-weight lead compounds.

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First Claim