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. 2008 Aug 6;2:75–80. doi: 10.2174/1874104500802010075

Table 1.

The Series of Chemical Compounds Under Investigation

Skeleton I
Compound R R1 R2 R3 R4 R5 X Activity, (IC50µ M)
1 H Me H - - - - 8.1
2 H H Me - - - - 0.10
3 H Cl H - - - - 0.55
4 H H Cl - - - - 0.0099
5 H NO2 H - - - - 3.0
6 H H NO2 - - - - 0.028
7 H H O-Me - - - - 0.35
8 H NH2 H - - - - 3.8
9 H H F - - - - 0.087
10 H Cl Cl - - - - 0.47
11 H O-Me O-Me - - - - 5.2
12 CH2-Ph Me H - - - - 3.7
13 CH2-Ph H Me - - - - 0.75
14 CH2-Ph H Cl - - - - 0.17
15 CH2-Ph NO2 H - - - - 1.6
16 CH2-Ph H NO2 - - - - 4.8
17 C7H15 Me H - - - - 0.39
18 C7H15 H Me - - - - 0.13
19 C7H15 H Cl - - - - 0.013
20 C7H15 H NO2 - - - - 0.29
21 C7H15 H O-Me - - - - 0.46
22 C7H15 H F - - - - 0.045
23 H H H - - - - 0.25
Skeleton II
Compound R R1 R2 R3 R4 R5 X Activity, (IC50μ M)
24 H H H H H H - 0.68
25 H NO2 H H H H - >100
26 H NO2 H H H H - 5.9
27 H H NO2 H H H - 67.5
28 H H NH2 H H H - 29
29 H H Cl H H H - 6.5
30 H H F H H H - 1.2
31 H H H O-Me H H - 1.6
32 H H H H O-Me H - 6.5
33 H H H H H O-Me - 4.3
34 H H H Me H H - 3.9
35 H H H H H Me - 4.6
36 H H H H F H - 0.43
37 H H H H Cl H - 5.4
38 CH2-Ph H H H H H - 7.1
39 Me H H H H H - 1.3
40 C7H15 H H H H H - 4.3
Skeleton III
Compound R R1 R2 R3 R4 R5 X Activity, (IC50µ M)
41 - - - - - - CH2-CH2 2.98
42 - - - - - - OCH2 245
43 - - - - - - SCH2 18.58
44 - - - - - - - 11.48