Table 2. KCNQ2/Q3 and KCNQ1 Activity of N-(6-Chloropyridin-3-yl) Benzamidesa.
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 |
NT, not tested.