Synthesis and antibacterial activity of C-12 pyrazolinyl spiro ketolides

A series of C-12 pyrazolinyl spiro ketolide derivatives were designed and synthesized. The C-12 modifications involved replacing the natural C-12 methyl group in clarithromycin core with different pyrazolinyl spiros via chemical synthesis. Potential anti-bacterial activities against both erythromycin-susceptible and erythromycin-resistant bacteria were reported.

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► A series of C-12 pyrazolinyl spiro ketolide derivatives were synthesized.
► New ketolides were found to have the improved anti-bacterial activities than erythromycin A and clarithromycin against Staphylococcus aureus strains, Staphylococcus. pneumonia and Haemophilus influenza strains.