Table 1.
Inhibitory activities of pterin-sulfa conjugates.
 | ||||||
|---|---|---|---|---|---|---|
| Cmpd | R |
BaDHPS in vitro FP Binding Inhibition IC50 (µM) |
Minimum Inhibitory Concentration E. coli K12, in µMb,c |
|||
| (−) PPia | (+) 2 mM PPia |
M9 media | M9 plus 5 µg/mL PABA |
M9 plus 20 µg/mL Methionine |
||
| 15 |  |
20.6±3.5 | 3.4±0.1 | 10.9 (0.8)c | 467 (263)c | 29 (1.5)c |
| 16 |  |
22.5±1.0 | 8.1± 0.7 | 28.3 (1.5) | >412 (249) | 47 (5.9) |
| 17 |  |
19.3±0.6 | 9.4± 0.7 | 17.1 (1.6) | >470 (666) | 78 (6.2) |
| 18 |  |
>62.5 | 2.5± 0.2 | 29.5 (2.7) | >471 (669) | 98 (6.3) |
| 19 |  |
26.8±3.0 | 1.9± 0.1 | 17.2 (1.6) | >412 (537) | 86 (3.4) |
| 20 |  |
15.2±0.6 | 11.5±0.8 | 34.3 (3.8) | >412 (>644) | 172 (10.1) |
| 21 |  |
17.8±0.8 | 11.3±1.1 | 197 (25) | 236 (>934) | 236 (50) |
| 22 |  |
18.6±0.8 | 17.1±1.2 | 136 (22) | >514 (>934) | >200 (58) |
| Ampicillin | ND | ND | 1.58 | 2 | 2.1 | |
| Chloramphenicol | ND | ND | 8.5 | 9.7 | 9.7 | |
| Trimethroprim | ND | ND | 1.7 | 1.4 | 0.7 | |
a
Present as sodium pyrophosphate. Average of 3 experiments, ±SEM.
b
Performed according to 24.
c
Corresponding values for parent sulfonamides shown in parentheses.