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In this work, a series of gatifloxacin-1,2,3-triazole-isatin hybrids tethered with methylene and acetyl (8a-n) were designed and synthesized, and the antibacterial activity profiles together with cytotoxicity were also investigated. The preliminary results indicated that all of the hybrids showed promising activity against a panel of Gram-positive and Gram-negative bacteria with MIC values in a range of ≤0.03 to 64 μg/mL. The cytotoxicity results demonstrated all hybrids displayed acceptable cytotoxicity towards VERO cells. Among these 14 hybrids, 8b and 8g with low cytotoxicity were no inferior to the parent gatifloxacin against Gram-positive and Gram-negative pathogens. Furthermore, we discussed the structure-activity relationship and structure-cytotoxicity relationship so as to point out the direction for further rationale design and modification of this series of hybrids.

Gatifloxacin-1,2,3-triazole-isatin hybrids tethered through methylene and acetyl and their antibacterial activities