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 |