Antibacterial activity against a selection of Gram-positive strains, toxicity data in HuDe cells and human red blood cells and therapeutic indices (TI) for the 10 synthesised lead compoundsa.
| MIC [μM] vs. Gram-positive bacteria | Toxicity [μM] | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| MRSA | MSSA | Se | Bs | En | En VRE | CC50 | HC50 | TI | |
| MnC5MeIm | 3.13–6.25 | 12.5–6.25 | 12.5 | 12.5–6.25 | 25 | 25 | 46.1 ± 0.1 | >200 | 7 |
| MnA3Clo | 1.56 | 1.56 | 3.13 | 3.13–1.56 | 6.25 | 3.13 | 37.1 ± 0.2 | 68 ± 15 | 24 |
| MnC8MeBeIm | 3.13–1.56 | 6.25 | 6.25 | 6.25 | 12.5 | 6.25 | 18.0 ± 0.2 | 77 ± 10 | 6 |
| MnC9MeBeIm | 3.13–1.56 | 3.13 | 6.25 | 3.13 | 12.5 | 12.5 | 16.8 ± 0.2 | 95 ± 13 | 5 |
| MnE2MeBeIm | 3.13–1.56 | 3.13 | 6.25–3.13 | 3.13 | 12.5 | 12.5 | 7.2 ± 0.3 | 49 ± 12 | 2 |
| MnG9MeBeIm | 0.78 | <0.78 | <0.78 | 3.13–1.56 | 6.25 | 6.25 | 85.2 ± 0.1 | 117 ± 12 | 109 |
| MnC1DMAP | 3.13–1.56 | 3.13–1.56 | 6.25 | 6.25–3.13 | 12.5 | 6.25 | 37.0 ± 0.2 | >200 | 12 |
| MnD8DMAP | 1.56 | 1.56–0.78 | 1.56 | 3.13–1.56 | 12.5 | 12.5 | 7.9 ± 0.2 | >200 | 5 |
| MnD9DMAP | 1.56 | 1.56 | 3.13 | 1.56 | 12.5 | 6.25 | 9.4 ± 0.2 | >200 | 6 |
| MnE6Quin | 6.25–3.13 | 6.25 | 12.5–6.25 | 6.25 | 50 | 25 | 36.3 ± 0.1 | >200 | 6 |
| VAN [μg mL−1] | 1 | 1 | 1 | 0.25 | 1 | 8 | |||
Antibacterial activity is displayed as MIC [μM]. MRSA – methicillin resistant S. aureus; MSSA – methicillin susceptible S. aureus; Se – S. epidermidis; Bs – Bacillus subtilis; En – Enterococcus spp En VRE – Enterococcus casselliflavus VRE, CC50 – HuDe cells; HC50 – human red blood cells; TI – therapeutic index, determined by dividing the lowest value between CC50 and HC50 with the lowest MIC value for each compound; VAN – vancomycin. MIC determined with n = 4 across two biological replicates.