Synthesis and in vitro activity of 1,2,4-triazole-ciprofloxacin hybrids against drug-susceptible and drug-resistant bacteria

A series of novel 1,2,4-triazole-ciprofloxacin hybrids was designed, synthesised and evaluated in vitro against drug-susceptible and drug-resistant bacteria. A significant part of the compounds obtained showed antibacterial activity higher than the activity of ciprofloxacin, both towards Gram-positive and Gram-negative species. Despite relatively small number of synthesised derivatives, it was possible to observe important dependences between their structure and activity.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Novel triazole-ciprofloxacin hybrids were designed and synthesised. ► Vast majority of the compounds were more active than ciprofloxacin. ► Preliminary structure–activity relationships (SAR) were analysed.