Table 3.
| |||
---|---|---|---|
Compd | R | Maximum activity (% rescue) |
EC50 (µM) |
10a | 2-Me | 6% ± 5% | - |
10b | 2-S-iPr | 30% ± 8% | >30 |
10c | 3-F | <0 | - |
10d | 3-NO2 | <0 | - |
10e | 3-NH2 | <0 | - |
10f | 3-OEt | 49% ± 11% | 26 ± 4.5 |
10g | 3-NHSO2Me | 24% ± 8% | 25 ± 2.1 |
10h | 4-Me | 25% ± 5% | 20 ± 5.4 |
10i | 4-O-propargyl | 54% ± 8% | >30 |
10j | 4SO2-NMe2 | 37% ± 6% | 19 ± 2.1 |
10k | 4-(N-pyrrolidinyl)methyl | 31% ± 7% | 11 ± 1.9 |
10l | 4-(N-piperidinyl)methyl | 87% ± 9% | 21 ± 3.5 |
10m | 3,4-Di-Cl | 42% ± 11% | 17 ± 6.1 |
10n | 3-Me-4-OMe | 56% ± 8% | 15 ± 3.2 |
10o | 2,3,4-trifluoro | 23% ± 6% | 9.9 ± 2.1 |
10p | 2,3,4,5-tetrafluoro | <0 | - |