Table 2. Antibacterial Activity and Hydrolytic Stability of C4-Substituted β-Lactam Analogs.
| PAO1aMIC | PBP3bkon | hydrolytic stabilityc | ||
|---|---|---|---|---|
| compd | (μg/mL) | (M–1 s–1) | t1/2 (h) | |
| 7b | trans-methyl | 0.5 | 1.7 × 105 | 93 ± 12 |
| 24a | cis-methyl | 1 | 1.6 × 104 | 76 ± 6.8 |
| 24b | cis-vinyl | 2 | 1.9 × 104 | 38 ± 4.1 |
| 25b | cis-ethyl | 1 | 8.8 × 103 | 94 ± 13 |
| 24c | trans-vinyl | 0.5 | 2.1 × 105 | 53 ± 2.8 |
| 24d | trans-ethyl | 0.5 | 3.6 × 105 | 98 ± 12 |
| 24e | cis-allyl | 8 | 5.9 × 103 | 126 ± 25 |
| 24f | cis-propyl | 4 | 7.4 × 103 | >150d |
| 24g | dimethyl | 8 | 1.1 × 104 | >150d |
a
PAO1 = P. aeruginosa ARC545.
b
P. aeruginosa PBP3.
c
pH = 7.4, 37 °C.
d
Not determined.