Synthesis, selective anti-Helicobacter pylori activity, and cytotoxicity of novel N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides

N-substituted-3-carboxamido-coumarin derivatives were prepared and evaluated for selective antibacterial activity against 20 isolates of Helicobacter pylori clinical strains, including five metronidazole resistant ones. Some of them possessed the best activity against H. pylori metronidazole resistant strains with MIC values lower than the drug reference (metronidazole). Furthermore, anti-inflammatory activity through the inhibition of the IL-8 production was investigated.

Graphical abstractA novel class of 20 N-substituted-3-carboxamido-coumarin derivatives were prepared and evaluated for their selective anti-Helicobacter pylori activity against several isolates of clinical strains, including five metronidazole resistant ones. Furthermore, a cytotoxic screening was carried out on the most active derivatives.Figure optionsDownload full-size imageDownload as PowerPoint slide