Table 2. Antibacterial activities of N-carboxy pyrrolidine analogs.
| Compound | S. aureus strain Newman (μg/mL)a | Methicillin Resistant S. aureus (MRSA) (μg/mL) | S. aureus strain RN4220 (μg/mL) | S. aureus strain RN4220 overexpressing SaFabI (μg/mL) | E. coli strain BW25113 ΔTolC (μg/mL) |
|---|---|---|---|---|---|
| 1 | 12.5 (41.7) | 25 | 12.5 | 50 * | 50 |
| 2 | 50 (176.5) | 100 | 50 | 200 | >200 |
| 3 | 50 (159.6) | 100 | 50 | 100 | >200 |
| 4 | 50 (165.9) | 100 | 50 | 200 | >200 |
| 5 | 100 | 100 | 100 | >200 | >200 |
| 6 | 50 (165.9) | >200 | 50 | >200 | >200 |
| 7 | 50 (150.9) | >200 | 50 | 50 | >200 |
| 8 | 25 (75.8) | 25 | 12.5 | 50 * | >200 |
| 10 | 50 (166.3) | 200 | 100 | 200 | >200 |
| 11 | 50 (163) | 100 | 50 | >200 | >100 |
| 12 | 6.25 18.2) | 25 | 12.5 | >200 * | 25 |
| 16 | 25 (69.1) | >200 | 25 | >200 * | >200 |
| 23 | >200 | >200 | >200 | >200 | 12.5 |
| 24 | 12.5 (34.2) | 25 | 12.5 | 50 * | 0.75 |
a
MIC values in μM concentrations are reported in brackets for compounds with MIC <50 μM
*
Compounds showing on-target activity against S. aureus
Compounds 9, 13-15, 17-22, 25-29 display MICs >200 μg/mL with all strains tested
All compounds were tested with native A. baumannii strain 2208 and E. coli strain BW25113 and found to display MICs > 200 μg/mL