TABLE 5.
Structures and in vitro activities of benzimidazoles
Compound | Ya | Ra |
C. albicans
|
C. neoformans
|
||
---|---|---|---|---|---|---|
MIC (μg/ml) | MFC (μg/ml) | MIC (μg/ml) | MFC (μg/ml) | |||
Amphotericin B | 1.0b | NTc | 1.0b | NT | ||
Fluconazole | 0.25 | NAd | 2.0 | NA | ||
48 | BzIm | OH | 3.12 | NT | 3.12 | NT |
49 | BzIm | OCH3 | 0.78 | NT | 3.12 | 3.12 |
50 | BzIm | OC2H5 | 0.78 | 12.5 | 1.56 | 1.56 |
51 | BzTHP | OH | 3.12 | 25 | 1.56 | 6.25 |
52 | BzAm | OH | 0.78 | 6.25 | 3.12 | 6.25 |
53 | BzAm | Am | 0.39 | 1.56 | ≤0.09 | 0.78 |
54 | BzIm | Im | 0.78 | 1.56 | 0.39 | 0.39 |
55 | BzAm | OCH3 | >100 | NT | 3.12 | >25 |
56 | BzTHP | THP | 0.78 | 1.56 | 0.19 | 0.39 |
57 | BzAm | OC2H5 | 0.78 | 1.56 | 1.56 | 1.56 |
58 | BzMPZ | OH | 25 | 50 | 100 | >100 |
59 | Im | OCH3 | 25 | NT | 50 | 100 |
60 | Am | Am | 100 | >100 | 25 | 50 |
61 | Am | OH | >100 | NT | >100 | >100 |
62 | Im | Im | 50 | >100 | 50 | NT |
63 | THP | THP | 50 | 100 | 25 | 50 |
64 | Am | O(CH2)3OPhAm | 0.39 | 0.78 | 0.19 | 0.78 |
65 | Am | O(CH2)4OPhAm | 0.39 | 3.12 | ≤0.09 | 1.56 |
66 | Am | O(CH2)5OPhAm | 0.78 | 1.56 | 0.39 | 6.25 |
67 | Am | OPhAm | 0.78 | 0.78 | 0.78 | 6.25 |