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. 2024 Feb 13;15(11):3907–3919. doi: 10.1039/d3sc05326a

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
a

Antibacterial activity is displayed as MIC [μM]. MRSA – methicillin resistant S. aureus; MSSA – methicillin susceptible S. aureus; SeS. epidermidis; BsBacillus subtilis; EnEnterococcus 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.