Table 1. m-Substituted Derivatives 1–10a.
code | R | % residual activity | IC50 (μM) |
---|---|---|---|
1 | 3-CF3 | 42.0 ± 6.3 | |
2 | 3-Cl | 101.6 ± 17.8 | |
3 | 3-OH | 70.4 ± 21.8 | |
4 | 3-CH3 | 103.9 ± 4.8 | |
5 | 3-NH2 | 65.8 ± 9.6 | |
6 | 3-CONH2 | 20.9 ± 4.3 | 31.4 ± 10.3 |
7 | 3-CONHCH3 | 84.0 ± 9.1 | |
8 | 3-SO2NH2 | 28.6 ± 6.8 | |
9 | 3-COOH | 27.2 ± 4.5 | |
10 | 3-CN | 3.1 ± 1.0 | 6.3 ± 0.9 |
Inhibitory effect is expressed as percentage of residual enzymatic activity (at 100 μM ligand concentration) for all compounds and half-maximal inhibitory concentrations (IC50, μM) only for the most active candidates (residual activity ≤ 25%).