Table 1.
a Biochemical potency data for analogs of 3.
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Compound | R1 | X | TbrPDEB1 (% inh) |
TbrPDEB1 (IC50 μM) |
TbrPDEB2 (IC50 μM) |
3 | CONMe2 | SO2 | 51 ± 3.9 | 24 ±1.7 | 29.8 ± 7.5 |
9a | CO2Me | S | 12 ±6.1 | - | - |
9b | H | S | 10.0b | ||
10a | CO2Me | SO2 | 70 ± 7.9 | 3.5 ± 0.3 | 15.1 ± 3.9 |
10b | H | SO2 | 21 ± 16 | - | - |
11 | CO2H | SO2 | 82 ± 10 | 2.9 ± 0.8 | 6.8 ± 0.6 |
12a | CONH2 | SO2 | 64 ± 7 | - | - |
12b | CONHMe | SO2 | 66 ± 6.1 | 31 ± 5.8 | - |
13 | CO2Me | NH | 84 ± 7.7 | 16 ± 1.7 | - |
All values are the mean of three or more replicates ± SEM.
n=1