Table 1.
Comp.# | pIC 50 a | n b | R | W | X | Y | Z |
---|---|---|---|---|---|---|---|
2 | 8.57 ± 0.15 | 8 | H | H | Cl | C | H |
4 | 8.14 ± 0.30 | 13 | OBu | H | H | N | H |
6 | 8.02 ± 0.20 | 5 | H | H | Cl | C | F |
7 | 8.71 ± 0.19 | 13 | H | F | Cl | C | H |
8 | 7.59 ± 0.23 | 3 | H | H | Me | N | H |
9 | 8.22 ± 0.30 | 9 | OMe | H | Cl | C | H |
10 | 7.92 ± 0.08 | 3 | OMe | H | H | N | H |
11 | 8.21 ± 0.21 | 4 | OEt | H | Cl | C | H |
12 | 7.37 ± 0.20 | 3 | OEtF | H | H | N | H |
13 | 8.19 ± 0.17 | 4 | OPr | H | Cl | C | H |
14 | 7.52 ± 0.16 | 5 | OPr | H | H | N | H |
15 | 8.75 ± 0.36 | 6 | OiPr | H | Cl | C | H |
16 | 6.42 ± 0.13 | 6 | OiPr | H | H | N | H |
17 | 7.53 ± 0.15 | 3 | MeOEt | H | H | N | H |
18 | 7.05 ± 0.25 | 7 | EtOMe | H | H | N | H |
19 | 7.19 ± 0.01 | 2 | OPrF | H | H | N | H |
20 | 7.0 ± 0.19 | 5 | OEtOMe | H | H | N | H |
21 | 8.1 ± 0.22 | 8 | OBu | H | Cl | C | H |
22 | 6.93 ± 0.05 | 2 | OBu | H | H | N | Cl |
23 | 6.88 ± 0.31 | 2 | PrOMe | H | H | N | H |
24 | 7.85 ± 0.30 | 8 | OMe-cycloPr | H | H | N | H |
aErrors are standard deviations. bn refers to number of independent repeat experimental measurements of pIC50, each repeat was performed in triplicate. The small compounds were: 2, 6, 7, 8, 9, and 10, and the large compounds were: 4, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23 and 24.