CONFORMATIONALLY CONSTRAINED C-BACKBONE CYCLIC PEPTIDES

摘要

Backbone cyclized peptide analogs that include at least one building unit of a C^alpha(omega-functionalized) amino acid that is constructed to include a spacer and a terminal functional group. The bridging groups are attached via alpha carbons of amino acid derivatives to provide novel non-peptide linkages. Also disclosed are novel C^alpha(omega-functionalized) amino acid building units, and methods of preparing them as well as the cyclized peptide analogs, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect the desired cyclization.