Novel C-7 Carbon Substituted Fourth Generation Fluoroquinolones Targeting N.Gonorrhoeae Infections

Fluoroquinolones (FQ) are a first-line antibacterial therapy, used to treat both
Gram-negative and Gram-positive bacterial infections. FQ efficacy is achieved by
disrupting the bacterial enzyme’s DNA gyrase and topoisomerase IV. There is
extensive SAR analysis of this class of antibiotics – both in terms of
microbiological activity1-3 and target related toxicity. Delafloxacin, a fourth
generation FQ has broad spectrum activity and reduced FQ related toxicity4-5
However, it has recently failed a Phase 3 clinical trial for treatment of N.
gonorrhoeae infections. This was due to lack of sufficient efficacy at the dose administered

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