Table 2. Inhibition of Human DAAO by Analogues of 11e.
compd | R2 | R3 | R4 | X1 | X2 | Y | Z | IC50 (μM)a |
---|---|---|---|---|---|---|---|---|
11e | H | H | H | H | H | O | N | 0.07 ± 0.01 |
11j | Cl | H | H | H | H | O | N | 0.10 ± 0.05 |
11k | H | Cl | H | H | H | O | N | 0.06 ± 0.02 |
11l | H | H | Cl | H | H | O | N | 0.04 ± 0.01 |
11m | F | H | H | H | H | O | N | 0.08 ± 0.03 |
11n | H | F | H | H | H | O | N | 0.06 ± 0.02 |
11o | H | H | F | H | H | O | N | 0.05 ± 0.02 |
11p | CH3 | H | H | H | H | O | N | 0.08 ± 0.03 |
11q | H | CH3 | H | H | H | O | N | 0.07 ± 0.02 |
11r | H | H | CH3 | H | H | O | N | 0.09 ± 0.02 |
11s | H | CF3 | H | H | H | O | N | 0.10 ± 0.02 |
11t | H | H | CF3 | H | H | O | N | 0.08 ± 0.04 |
11u | OCH3 | H | H | H | H | O | N | 0.27 ± 0.07 |
11v | H | OCH3 | H | H | H | O | N | 0.12 ± 0.03 |
11w | H | H | OCH3 | H | H | O | N | 0.12 ± 0.03 |
15u | OH | H | H | H | H | O | N | 0.09 ± 0.04 |
15v | H | OH | H | H | H | O | N | 0.16 ± 0.05 |
15w | H | H | OH | H | H | O | N | 0.11 ± 0.03 |
11x | H | OPh | H | H | H | O | N | 0.24 ± 0.05 |
11y | H | H | OPh | H | H | O | N | 0.08 ± 0.02 |
11z | H | H | Ph | H | H | O | N | 0.05 ± 0.02 |
19e | H | H | H | CH3 | H | O | N | 3.3 ± 0.6 |
19f | H | H | H | F | F | O | N | 0.40 |
22 | H | H | H | O | O | O | N | 0.85 ± 0.13 |
23 | H | H | H | OH | H | O | N | 0.47 ± 0.23 |
30 | H | H | H | H | H | S | N | 0.05 ± 0.01 |
32 | H | H | H | H | H | O | CH | 0.08 ± 0.01 |
Values are mean ± SD of at least four experiments except for compound 19f (n = 2).