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. Author manuscript; available in PMC: 2013 Aug 9.
Published in final edited form as: J Med Chem. 2012 Jul 26;55(15):6975–6979. doi: 10.1021/jm300700v

Table 3.

SAR evaluation of the phenyl substituent on the inhibitor and activator scaffolds.

graphic file with name nihms-396409-t0019.jpg
KCNQ2 (μM)10
Entry R Ri IC50 EC50
19 3,4-dimethoxy Et 20.23 ± 4.89
20 3,4-difluoro Et 0.17 ± 0.02
21 H 1.73 ± 0.34
22 3-fluoro Et 0.36 ± 0.03
23 H 0.49 ± 0.12
24 3-methyl Et 0.33 ± 0.05
25 H 1.32 ± 0.29
26 4-fluoro Et 0.13 ± 0.03
27 H 0.70 ± 0.82
28 3,4-dichloro Et 0.47 ± 0.08
29 H 1.07 ± 0.34
30 2-chloro Et 3.31 ± 0.87
31 H 0.95 ± 0.27
32 3-trifluoromethyl Et 0.39 ± 0.14
33 H 0.35 ± 0.21
34 3-methoxy Et 0.12 ± 0.03
35 H 2.35 ± 2.25
36 3-chloro Et 0.24 ± 0.04
37 H 0.17 ± 0.12
38 4-methoxy Et 0.38 ± 0.06
39 H 1.75 ± 0.59
40 4-chloro Et 0.28 ± 0.03
41 H 0.80 ± 0.31
42 2-fluoro Et 0.44 ± 0.09
43 H (26.6%)