Novel C-7 Carbon Substituted Fourth Generation Fluoroquinolones Targeting N.Gonorrhoea 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 topoisimerase IV. There is extensive SAR analysis of this class of antibiotics-both in terms of microbiological activity 1-3 and target related toxicity. Delafloxacin, a fourth generation FQ has broad spectrum activity and reduced FQ related toxicity 4-5. 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.