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. 2020 Feb 7;9(2):69. doi: 10.3390/antibiotics9020069

Table 1.

General overview of the best FtsZ inhibitors. MIC—minimum inhibitory concentration; IC50—half maximal inhibitory concentration; STD—saturation transfer difference; ITC—isothermal titration calorimetry.

Site Class (Figure) Best Compounds MICs Evidence for FtsZ Inhibition References
2.1. GTP-binding site 2.1.1. Pyrimidines (3) N6–N8 S. aureus: 4–8 μM
Enterococcus faecalis: 4–8 μM
E. faecium: 4–8 μM

  • Polymerization assay;

  • GTPase activity assay;

  • Microscopy evaluation.

 [14,15]
2.1.2. Zantrins (4) N11 S. aureus: 5 μM
E. coli: DRC39: 10 μM

  • IC50 evaluation;

  • Molecular modeling.

 [16,17,18,19]
2.1.3. Chrysophaentins (5) N17 S. aureus: 5–9 μM
E. faecium: 5–6 μM

  • Polymerization assay;

  • GTPase activity assay;

  • STD-NMR;

  • Molecular modeling.

 [20,21,22]
2.1.4. GTP analogues and derivatives (6) N23-N26 B. subtilis: 8.5 μM
S. aureus: 5–50 μM

  • Microscopy evaluation;

  • Sedimentation assay;

  • Polymerization assay;

  • Molecular modeling.

 [23,24]
2.2. Interdomain site 2.2.1. Benzamides (7) I3; I4; I7–I12 B. subtilis: <1 μM
S. aureus: 1.6–2.8 μM
E. coli N43: 19–42 μM

  • Polymerization assay;

  • GTPase activity assay;

  • Microscopy evaluation;

  • Molecular modeling;

  • X-ray crystallography.

 [25,26,27,28,29,30,31,32,33,34,35,36,37,38,39,40,41,42,43,44,45,46,47,48,49]
2.2.2. Berberine analogues and derivatives (8) I20–I22 B. subtilis: 2.8–8 μM
S. aureus: 2.7–8 μM
E. coli: 5.5 μM

  • Polymerization assay;

  • GTPase activity assay;

  • Microscopy evaluation;

  • STD-NMR;

  • ITC.

 [50,51]
2.2.3. Phenantridium derivatives (9) I25 B. subtilis: 12.7 μM
S. aureus: 51 μM

  • Microscopy evaluation;

  • Polymerization assay;

  • Molecular modeling.

 [52]
2.2.4. Indoles (10) I26 B. subtilis: 4.5 μM
S. aureus: 4.5–9.1 μM

  • Polymerization assay;

  • GTPase activity assay;

  • Microscopy evaluation.

 [53]