Antibiotics

Coumarins

Activity: DNA gyrase and topo IV inhibitors. Inhibit the hydrolysis of ATP by binding as a site overlapping the ATP-binding site, acting as competetive inhibitors.

Source: Naturally occuring products of Streptomyces species

• Novobiocin

Formula:     C₃₁H₃₆N₂O₁₁                M. Wt.:         612.6 g/mol

Solubility:    Soluble in water, ethanol and DMSO (all at 100 mg/ml).

• Clorobiocin

Formula:     C₃₅H₃₇N₂O₁₁Cl             M. Wt.:         697.1 g/mol

Solubility: Insoluble in water, poorly soluble in ethanol (1 mg/ml) and soluble in DMSO (> 100 mg/ml).

• Coumermycin A1

Synonyms:  Notomycin

Formula:     C₅₅H₅₉N₅O₂₀                M. Wt.:         1109.4 g/mol

Solubility:

Quinolones

Activity:  DNA gyrase and topo IV inhibitors. Interfere with DNA chain breakage and reunion.

Source:   Synthetic compounds.

• Naladixic Acid

Formula:      C₁₂H₁₂N₂O₃                 M. Wt.:         232.2 g/mol

Solubility:    Soluble in water (100 mg/ml).

• Ciprofloxacin

Formula:      C₁₇H₁₈N₃O₃F                M. Wt.:         331.3 g/mol

Solubility:    Soluble in water (> 30 mg/ml), soluble in ethanol (< 10 mg/ml) and DMSO (< 10 mg/ml).

• Simocyclinone

Activity:  DNA gyrase inhibitors. Inhibits early stage of catalytic cycle, inhibiting binding of DNA to enzyme.

Source:   Streptomyces antibioticus

Formula:      C₄₆H₄₂NO₁₈Cl         M. Wt.: 932.3 g/mol

Solubility:    Poorly soluble in water, soluble in DMSO (10 mg/ml).