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C-Terminal lactamization of peptides
Solid-phase synthesis of peptides (SPPS) with release through formation of C-terminal gamma-, delta-, or epsilon-lactams is presented. The natural products ciliatamide A and C were synthesized in up to 90% yield. Peptides carrying C-terminal lactams were shown to possess increased bio-stability and comparable biological activity as compared to the parent non-lactamized peptide amides.
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