CONFORMATIONALLY CONSTRAINED C-BACKBONE CYCLIC PEPTIDES

摘要

The present invention provides novel backbone cyclized peptide analogs comprising at least one building unit, which is a C< ALPHA >( omega -functionalized) amino acid constructed to include a spacer and a terminal functional group. The cyclized peptide analogs are formed by means of bridging groups attached via the alpha-carbons of amino acid derivatives to provide novel non-peptidic linkages. The present invention further provides certain novel C< ALPHA >( omega -functionalized) amino acid building units, methods of preparing the C< ALPHA >( omega -functionalized) amino acid building units, and methods of preparing the novel backbone cyclized peptide analogs by incorporating one or more of these C< ALPHA >( omega -functionalized) amino acid building units into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations.