| 摘要 |
<p>A 'capped' phosphonamide C1-C6 alkyl ester linkage unit for joining peptides is disclosed. The linkage unit is substantially isosteric and isocoulombic as compared to conventional peptide backbone structures. The 'capping' of the phosphonamide by the C1-C6 alkyl ester causes the linkage unit to be acid stable. When incorporated into a peptide, the phosphonamide C1-C6 alkyl ester linkage unit becomes resistant to cleavage by aspartic proteinase. Accordingly, the phosphonamide C1-C6 alkyl ester linkage unit enhances and/or facilitates the aspartic proteinase inhibition activity of peptides into which it is incorporated.</p> |
