Novel chemistry

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Pradofloxacin, the active ingredient of Veraflox®, is a novel synthetic antimicrobial of the fluoroquinolone class and the 1st third-generation agent developed exclusively for veterinary medicine.

The molecule differs from other fluoroquinolones at three strategic positions, thus increasing favourable performance characteristics:

  1. The cyclopropyl group in position N1 controls overall antibacterial potency, contributes to Gram-negative activity and is regarded as the substituent of choice in this position.
  2. The presence of a pyrrolidino-piperidine substituent at the position 7 is associated with high Gram-negative activity and considerably greater Gram-positive activity, for both wild-type strains and those with reduced fluoroquinolone susceptibility. The addition also contributes to more favourable pharmacokinetics as higher lipophilicity and a longer half-life.
  3. The cyano group at position 8 has been shown to enhance the activity against first step fluoroquinolone-resistant strains of Staphylococcus aureus and Escherichia coli as shown by respectively reduced Mutant Prevention Concentration (MPC) values. Furthermore this substituent provides a moderate to absent phototoxic potential as well as the absence of retinal toxicity. In addition, activity against anaerobic bacteria involved in periodontal disease is markedly enhanced.
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