| abstract |
A novel backbone cyclized peptide analog is provided. It is formed by a bridging group linked through the alpha nitrogen of an amino acid derivative that produces a novel non-peptide bond. The new building unit is a N α / (ω-functionalized) amino acid constructed to contain a spacer and a terminal functional group. One or more of these N α / (ω-functionalized) amino acids are incorporated into the peptide sequence, preferably during solid phase peptide synthesis. Reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect main chain-main chain cyclization or main chain-side chain cyclization. The peptide analog is exemplified by a biologically active backbone cyclized bradykinin antagonist, and another embodiment is a somatostatin analog having one or two ring structures with backbone cyclization. [Selection figure] None |