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. Author manuscript; available in PMC: 2010 Dec 14.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Oct 25;19(24):6851–6854. doi: 10.1016/j.bmcl.2009.10.090

Table 1.

Aryl ring optimizationa

graphic file with name nihms-161255-t0002.jpg
R1 R2 R3 R4 Ki (μM)
20 H H H H 24.0 ± 0.9
22 F H H H >100
23 Cl H H H 68.0 ± 6.0
24 CF3 H H H 54.8 ± 14.5
25 Br H H H 44.6 ± 7.4
26 H F H H 41.8 ± 5.8
27 H Cl H H 34.9 ± 3.5
28 H Br H H 18.2 ± 0.9
29 H CF3 H H 10.7 ± 1.2
30 H H F H 22.7 ± 3.2
31 H H CF3 H 18.5 ± 2.5
32 H H Cl H 16.8 ± 7.0
33 H H Br H 10.3 ± 1.0
34 H CF3 F H 11.4 ± 0.3
35 H CF3 Cl H 6.0 ± 0.4
36 H CF3 Br H 4.9 ± 1.7
37 H CF3 H CF3 3.3 ± 0.6
38 H CF3 Br CF3 1.4 ± 0.3
a

Ki values were determined using at least four independent measurements.