Table 2. Inhibitory Data of Bis-triazoles 15–17 and Hydroxamates 24b,c under Increased ThDP Levels.
|
Inhibition (%)a |
||||
|---|---|---|---|---|
| Compound | PDHc E1b | Yeast PDCc | OGDHc E1b | POb |
| OxThDP 7b | 75 ± 3 | 63 ± 3 | 41 ± 4 | 32 ± 5 |
| 15a | <20 | Insoluble | <20 | <20 |
| 15b | 40 ± 4 | Insoluble | <20 | <20 |
| 15c | 75 ± 4 | Insoluble | <20 | <20 |
| 16a | <20 | Insoluble | <20 | <20 |
| 16b | 43 ± 2 | Insoluble | <20 | <20 |
| 16c | 79 ± 2 | Insoluble | <20 | <20 |
| 17a | <20 | Insoluble | <20 | <20 |
| 17b | 45 ± 3 | Insoluble | <20 | <20 |
| 17c | 82 ± 4 | Insoluble | <20 | <20 |
| 24b | 70 ± 3 | 42 ± 4 | 78 ± 3 | 27 ± 4 |
| 24c | 73 ± 4 | 37 ± 4 | 82 ± 2 | 24 ± 4 |
a
Data are the means of measurements in three technical replicates. Compared to Table 1, the assays here were conducted with an increase in [ThDP]:[inhibitor] from 1:5 to 1:2.
b
[Compound] = 250 μM, [ThDP] = 125 μM.
c
[Compound] = 1500 μM, [ThDP] = 750 μM; compounds insufficiently soluble were excluded.