Table 1.
Example | R1 | R2 | R3 | R4 | R5 | IC50 (μM) or Remaining Activity % (RA%) at 10 μM (bold) | |
---|---|---|---|---|---|---|---|
PAO1-L | PA14 | ||||||
7 | H | 4-Cl | H | H | H | 0.98 ± 0.02 | NA |
8 | Br | 4-Cl | H | H | H | 1.99 ± 0.23 | 1.60 ± 0.16 |
9 | H | H | H | H | H | NA | NA |
10 | Br | H | H | H | H | NA | NA |
11 | H | 3-Cl | H | H | H | RA% 34 ± 7.3 | NA |
12 | Br | 3-Cl | H | H | H | RA% 43 ± 20.2 | NA |
13 | H | 3,4-dichloro | H | H | H | NA | NA |
14 | Br | 3,4-dichloro | H | H | H | 3.1 ± 0.52 | 7.58 ± 0.82 |
15 | H | 4-F | H | H | H | NA | NA |
16 | Br | 4-F | H | H | H | 1.36 ± 0.21 | NA |
17 | H | 4-Me | H | H | H | 1.86 ± 0.01 | NA |
18 | Br | 4-Me | H | H | H | RA% 32 ± 6.2 | NA |
19 | H | 4-OMe | H | H | H | NA | NA |
20 | Br | 4-OMe | H | H | H | NA | NA |
21 | H | 4-OCF3 | H | H | H | RA% 29 ± 6 | NA |
22 | Br | 4-OCF3 | H | H | H | RA% 23 ± 9 | NA |
23 | H | 4-(cyanomethyl) | H | H | H | 0.62 ± 0.10 | 2 ± 0.17 |
24 | H | 4-phenoxy | H | H | H | 0.38 ± 0.06 | 0.35 ± 0.06 |
25 | Br | 4-phenoxy | H | H | H | 4.36 ± 0.42 | NA |
26 | H | 4-Br | H | H | H | 1.71 ± 0.26 | 1.35 ± 0.19 |
27 | Br | 4-Br | H | H | H | 23 ± 9 | NA |
28 | H | 4-(pyrimidin-2-yloxy) | H | H | H | 1.04 ± 0.12 | 1.33 ± 0.33 |
38 | H | 2-Cl | H | H | H | NA | NA |
39 | Br | 2-Cl | H | H | H | NA | NA |
40 | H | 4-(pyridin-2-yloxy) | H | H | H | 0.25 ± 0.12 | 0.34 ± 0.03 |
41 | H | 4-Cl | Me | H | H | NA | NA |
42 | H | 4-Cl | H | Me | Me | NA | NA |
43 | H | 4-Cl | H | Me | H | NA | NA |
44 | H | 4-Cl | Me | H | Me | NA | NA |
M64 | 0.32 ± 0.14 | 1.22 ± 0.34 |
Data shown are based on n = 9. NA, not active at 10 M concentration. Bold values represent percentage of remaining activities at 10 μM concentration.