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. Author manuscript; available in PMC: 2015 Apr 15.
Published in final edited form as: Curr Top Med Chem. 2012;12(7):672–693. doi: 10.2174/156802612799984535

Table 10.

SAR study on arylamides.

Compound X n R1 R2 IC50 (μM)
a1 N 0 H H 38.86 ± 1.35
a2 N 0 4-CH3 H 16.64 ± 0.49
a3 N 0 4-CH3 3-CF3 6.26 ± 0.33
a4 N 0 4-CH3 3-CI 3.07 ± 0.48
a5 N 0 3-CH3 3-CI 9.43 ± 0.80
a6 N 0 3-CH3 4-NO2 15.47 ± 1.52
a7 N 0 3, 4-Me2 3-CI 0.99 ± 0.03
a8 N 0 3, 4-Me2 3-CF3 1.85 ±0.08
a9 N 0 4-i-Pr 3-CI >100
a10 N 0 4-t-Bu 3-CI >100
a11 N 0 4-t-Bu 3-CF3 >100
a12 N 0 4-t-Bu 4-CH3,
3-CI
>100
a13 N 0 2-F 3-CI 13.87 ± 1.03
a14 N 0 4-F 3-CI 9.74 ± 0.62
a15 N 0 3-CI 3-CI 6.73 ± 0.27
a16 N 0 3, 4-CI2 3-CI 6.05 ± 0.58
a17 N 0 3, 4-CI2 H 17.62 ± 1.24
a18 N 1 H H 31.50 ± 1.65
b1 C 1 3-CI H 7.74 ± 0.25
b2 C 1 2-F H 14.11 ± 0.42
b3 C 1 4-CH3 H 5.16 ± 0.45
b4 C 1 3-CH3 H 7.39 ± 0.38