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Activity of representative dipeptidyl inhibitors (I): Aldehydes and bisulfite adducts.
| R | R1 | Z | IC50 (μM) | EC50 (μM) | |
|---|---|---|---|---|---|
| 1 | H | Isobutyl | CHO | 0.6 | 0.2 |
| 2 | CH(OH)SO3− Na+ | 0.8 | 0.3 | ||
| 3 | Cyclohexylmethyl | CHO | 0.3 | 0.06 | |
| 4 | CH(OH)SO3− Na+ | 0.4 | 0.06 | ||
| 5 | Butyl | CHO | 0.87 | ND | |
| 6 | m-Cl | Isobutyl | CHO | 0.9 | 0.1 |
| 7 | CH(OH)SO3− Na+ | 4.3 | 0.1 | ||
| 8 | Cyclohexylmethyl | CHO | 0.1 | 0.02 | |
| 9 | CH(OH)SO3− Na+ | 0.1 | 0.02 |
