Table 1.
Structures and IC50 values of the (β-lactam-based PSA inibitors developed by Adlington et al. (1997, 2001).
| ||||
|---|---|---|---|---|
| Compound | R1 | R2 | R3 | IC50 (μM) |
| 1 | H | CO2Bn | CO2H | 8.98 ± 0.1 |
| 2 | H | P-CO2CH2-C6H4-CO2H | CO2H | 5.84 ± 0.9 |
| 3 | H | H | CO2H | 24.3 ± 3.9 |
| 4 | H | CO2H | CH2NH2-TFA | 1.34 ± 0.1 |
| 5 | H | CO2Bn | H | 1.43 ± 0.2 |
| 6a | OH | CO2Bn | H | 0.348 ± 0.1 |
| 7b | OH | CO2Bn | H | 0.226 ± 0.01 |
Racemic mixture of compounds.
Homochiral 3S4S enantiomer.