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Synthesis and Evaluation of Thiazolidine Amide and N‐Thiazolyl Amide Fluoroquinolone Derivatives

In an effort to develop new fluoroquinolones, we synthesized eight compounds and tested them against a panel of bacteria. The design of these compounds was guided by the introduction of the isothiazoloquinolone motif. The three most active compounds in this series, 8–10, demonstrated good antibacterial activity against methicillin‐sensitive Staphylococcus aureus and healthcare‐acquired methicillin‐resistant Staphylococcus aureus (MIC 0.62–6.3 µg/mL). Further, when these three active compounds were tested for their inhibitory effects on bacterial enzymes, compound 9 was the most effective agent exhibiting IC50 values of 33.9 and 116.5 μM in the S. aureus deoxyribonucleic acid (DNA) gyrase supercoiling and topoisomerase IV decatenation assays, respectively.