Table 1.
Enzyme Inhibition Data for Substituted Benzimidazolesa
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---|---|---|
compd | X | % inhibitionb (1 μM) |
(A) 5, 6, or 7-Methyl-Substituted | ||
1-(2,6-Difluorobenzyl)-2-(2,6-difluorophenyl)benzimidazoles | ||
2 | H | 50 |
1 | 4-CH3 | 71 |
41 | 5-CH3 | 22 |
42 | 6-CH3 | 42 |
43 | 7-CH3 | 1 |
45 | 4,5-diCH3 | 26 |
46 | 4,6-diCH3 | 37 |
(B) 4, 5, or 6-Substituted | ||
1-(2,6-Difluorobenzyl)-2-(2,6-difluorophenyl)benzimidazoles | ||
54 | 4-Br | 78 |
38 | 5-Br | 43 |
55 | 4-Cl | 75 |
39 | 5-Cl | 48 |
40 | 6-Cl | 69 |
48 | 4-NO2 | 51 |
49 | 5-NO2 | 30 |
Enzyme assays done with WT RT.
% inhibition is the average of two experiments done in triplicate.