Table 1. Anti-fondaparinux Activities of N-Terminal Truncations, Side Chain Modifications, and C-Terminal Truncations of SalAA Foldamersa.
| compound | sequence | FXa EC50 (μM) |
|---|---|---|
| N-Terminal Modifications | ||
| 8 | H2N-(Lys-Sal)3-CONH2 | inactive |
| 5 | Sal-(Lys-Sal)3-CONH2 | 6.8 |
| 6 | Ac-Sal-(Lys-Sal)3-CONH2 | 2.3 |
| 1 | Lys-Sal-(Lys-Sal)3-CONH2 | 3.6 |
| 1a | H2N-(d-Lys-Sal)4CONH2 | 3.0 |
| 7 | H2N-(d-Cit-Sal)4-CONH2 | inactive |
| C-Terminal Modifications | ||
| 1 | H2N-(Lys-Sal)4-CONH2 | 3.6 |
| 2 | H2N-(Lys-Sal)4-COOH | inactive |
| 3 | H2N-(Lys-Sal)4-COOCH3 | 11 |
| 4 | H2N-(Lys-Sal)4-CONH-(CH2)2-COOH | 6.0 |
a
Average standard deviation was ±9%.