Skip to main content
. 2011 Mar 31;2(6):481–484. doi: 10.1021/ml200053x

Table 2. KCNQ2/Q3 and KCNQ1 Activity of N-(6-Chloropyridin-3-yl) Benzamidesa.

graphic file with name ml-2011-00053x_0005.jpg

compd no. R-substituent KCNQ2/Q3 EC50 (μM) KCNQ1 IC50 (μM)
12 3,4-F2 0.38 41
16 4-Cl 0.38 15
17 H 1.6 >100
18 2-F >10 NT
19 3-F 1.1 77
20 4-F 0.98 66
21 3-CF3 0.39 5.8
22 4-CF3 0.32 2.9
23 4-Ph 0.26 >30
24 3-OCH3 5.5 NT
25 3,4 (CH3)2 0.69 >100
26 3,4-Cl2 0.67 17
27 3-Cl 0.27 41
28 3-F, 4-Cl 0.08 15
29 3-CF3, 4-F 0.42 3.4
30 4-SO2NH2 >10 NT
31 3-F, 4-CF3 0.37 3.4
32 3-Cl, 4-F 0.19 22
33 3-F, 4-CH3 0.28 33
34 3-CN >10 NT
35 2,3-F2 >10 NT
36 4-OC6H5 0.01 1.9
37 3-F, 4-CN 1.1 51
38 3-F, 4-OCH3 3.2 >100
39 3-F, 4-OEt 0.57 >100
40 3-F, 4-OiPr 0.17 >100
41 3-F, 4-OC6H5 0.03 1.3
42 3-F, 4-(4F−C6H5S) 0.08 >100
43 3-F, 4-(4F−C6H5SO2) 0.07 >100
44 3-F, 4-(4F−C6H5CH2S) 1.6 >100
45 3-F, 4-(4F−C6H5CH2SO2) 0.16 >100
46 3-F, 4-SiPr 0.11 5.8
47 3-F, 4-SiBu 0.14 >100
48 3-F, 4-SO2iBu 0.26 54
49 3-F, 4-NHCH2CH2C6H5 0.18 >100
a

NT, not tested.