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. 2015 Aug 26;58(18):7258–7272. doi: 10.1021/acs.jmedchem.5b00482

Table 2. Inhibition of Human DAAO by Analogues of 11e.

graphic file with name jm-2015-00482r_0013.jpg

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
a

Values are mean ± SD of at least four experiments except for compound 19f (n = 2).