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. 2018 Dec 19;10(1):27–33. doi: 10.1021/acsmedchemlett.8b00315

Table 2. Structures of N-2/3 Derivatives 8, 10, and 13 and Their Effects on the KCNQ2, 4, and 5 Channels.

graphic file with name ml-2018-00315a_0008.jpg

      I/I0a
Cpds R2 R3 KCNQ2 KCNQ4 KCNQ5
8a Me Me 1.37 ± 0.11 4.77 ± 0.44 2.89 ± 0.07
8b allyl allyl 0.67 ± 0.02 2.21 ± 0.11 5.26 ± 0.53
8c nPr nPr 0.78 ± 0.04 2.58 ± 0.56 2.75 ± 0.84
8d iPr iPr 0.35 ± 0.04 1.33 ± 0.06 3.11 ± 0.93
8e nBu nBu 0.77 ± 0.02 2.75 ± 0.40 4.13 ± 1.09
8f iBu iBu 0.83 ± 0.04 1.52 ± 0.17 1.73 ± 0.10
8g tBu tBu 1.00 ± 0.09 3.05 ± 0.74 5.32 ± 0.39
8h cyclopropyl cyclopropyl 0.64 ± 0.03 1.51 ± 0.04 2.55 ± 0.38
8i cyclobutyl cyclobutyl 0.26 ± 0.06 1.21 ± 0.09 1.33 ± 0.23
8j cyclopentyl cyclopentyl 0.21 ± 0.05 0.88 ± 0.07 1.25 ± 0.14
8k Ph Ph 0.91 ± 0.02 1.22 ± 0.05 1.16 ± 0.04
8l Bn Bn 1.25 ± 0.01 3.02 ± 0.28 3.57 ± 0.31
10a Et Me 0.61 ± 0.05 2.56 ± 0.47 3.34 ± 0.54
10b Et Allyl 0.96 ± 0.04 3.68 ± 0.36 4.67 ± 0.69
10c Et nPr 1.07 ± 0.03 3.95 ± 0.89 5.81 ± 0.62
10d Et iPr 0.94 ± 0.06 5.01 ± 0.83 5.71 ± 0.34
10e Et nBu 1.06 ± 0.03 4.16 ± 0.60 3.62 ± 0.31
10f Et iBu 1.04 ± 0.04 5.19 ± 0.64 4.84 ± 0.32
10g Et tBu 1.16 ± 0.04 6.37 ± 0.84 4.58 ± 0.32
10h Et Bn 0.97 ± 0.15 1.27 ± 0.03 2.57 ± 0.67
13 tBu Et 1.07 ± 0.06 7.71 ± 0.50 4.59 ± 0.56
a

The testing concentration was 10 μM. Each compound was tested in more than four cells.