Table 1.
| ||||
---|---|---|---|---|
Compound | R1 | R2 | R3 | R4 |
1 * | NHMe | Me | H | H |
2 * | NHcyclopropyl | Me | H | H |
3 | NHcyclopentyl | Me | H | H |
4 | NHPh | Me | H | H |
5 | NH2 | Me | CF3 | H |
6 | NH2 | Ph | H | H |
7 | NH2 | i-Pr | H | H |
8 | NH2 | 1-methylpiperidine-4-yl | H | H |
9 | NH2 | 2-(piperidin-1-yl)-ethyl | H | H |
10* | NH2 | Me | H | m-CF3 |
11 | NH2 | Me | H | p-CF3 |
12 | NH2 | Me | Ac | H |
13 | NH2 | Me | H | m-Ac |
14 | NH2 | Me | OMe | H |
15 | NH2 | Me | H | m-OMe |
16 | NH2 | Me | H | p-OMe |
17 | NH2 | Me | NO2 | H |
18 | NH2 | Me | H | m-NO2 |
19 | NH2 | Me | Me | H |
20 * | NH2 | Me | NHMe | H |
21 | NH2 | Me | i-Pr | H |
22 * | NH2 | Me | COOMe | H |
23 * | NH2 | Me | CONH2 | H |
24 | NH2 | Me | SO2NH2 | H |
25 | NH2 | Me | Ph | H |
26 * | NH2 | Me | OPh | H |
27 | NH2 | Me | benzyl | H |
28 * | NH2 | Me | NHPh | H |
29 | NH2 | Me | benzoyl | H |
30 * | NH2 | Me | SPh | H |
31 | NH2 | Me | Ac | 3′-(4-methyl-piperazin-1-yl) |
32 * | NH2 | Me | Ac | 4′-(4-methyl-piperazin-1-yl) |
33 | NH2 | Me | Ac | 5′-(4-methyl-piperazin-1-yl) |
34 | NH2 | Me | OMe | 4′-(4-methyl-piperazin-1-yl) |
35 * | NH2 | Me | OMe | 5′-(4-methyl-piperazin-1-yl) |
36 | OEt | Me | H | H |
37 | NH2 | Me | NH2 | H |
38 | NH2 | Me | NHAc | H |
39 | NH2 | Me | OCF3 | H |
40 | NH2 | Me | OCF3 | |
41 * | NH2 | Me | OCF3 | |
42 | NH2 | Me | OCF3 | |
43 | NH2 | Me | OCF3 | |
44 | NH2 | Me | OCF3 | |
45 | NH2 | Me | OCF3 | |
46 * | NH2 | Trityl | OCF3 | |
47 | NH2 | H | OCF3 | |
48 * | NH2 | 2-Fluoro-ethyl | OCF3 | |
49 | NH2 | Ethyl | OCF3 | |
50 * | NH2 | 2-Methoxy-ethyl | OCF3 | |
51 | NH2 | 2-Chloro-ethyl | OCF3 | |
52 | NH2 | Vinyl | OCF3 | |
53 * | NH2 | Me | OCF3 | |
54 | NH2 | Me | OCF3 | 5′-NH2 |
55 | NH2 | Me | OCF3 | |
56 * | NH2 | Me | OCF3 | |
57 | NH2 | Me | OCF3 | |
58 | NH2 | Me | OCF3 | |
59 | NH2 | Me | OCF3 | |
60 | NH2 | Me | OCF3 | |
61 | NH2 | Me | OCF3 | |
62 * | NH2 | Me | OCF3 | |
63 | NH2 | Me | OCF3 | |
64 * | NH2 | Me | OCF3 | |
65 | NH2 | Me | OCF3 | |
66 * | NH2 | Me | OCF3 | |
67 | NH2 | Me | OCF3 | |
68 | NH2 | Me | OCF3 | |
69 | NH2 | −(CH2)3–N–(CH3)2 | OCF3 | |
70 * | NH2 | OCF3 | ||
71 | NH2 | − (CH2)2–NH2 | OCF3 | |
72 | NH2 | − (CH2)3–NH2 | OCF3 | |
73 | NH2 | − (CH2)2–OH | OCF3 |
Compounds in test set.