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. 2014 May 13;9(7):1536–1544. doi: 10.1021/cb5001586

Table 2. SAR of Pyridine with a 4-Substituted Phenyl Ring.

graphic file with name cb-2014-001586_0007.jpg

analog R1 R2 μM
3 2-Cl Cl 0.04 ± 0.01
14 3-Cl Cl 0.13 ± 0.04
15 5-Cl Cl 0.01 ± 0.004
16 2-CF3 Cl 0.01 ± 0.005
17 2-CN Cl 0.18 ± 0.05
18 2-CH3 Cl 0.25 ± 0.04
19 3-CH3 Cl 0.25 ± 0.09
20 3-CF3 Cl 2.4 ± 1.2
21 2-Cl, 3-CF3 Cl 0.62 ± 0.08
22 2-CN, 3-CH3 Cl 0.18 ± 0.02
23 3-CN Cl 2.5 ± 0.5
24 H Cl 0.27 ± 0.03
4 2-CF3 F 0.02 ± 0.01
25 2-CH F 0.13 ± 0.02
26 2-CN, 3-CH3 F 0.13 ± 0.07
27 2-Cl, 3-CF3 F 0.74 ± 0.28
28 2-Cl, 3-CF3 CF3 2.3 ± 1.9
29 2-CF3 CF3 0.14 ± 0.06
a

Average of at least three replicates ± standard deviation.