Synthesis and antibacterial activity of 9-substituted minocycline derivatives

A number of 9-acylamino and 9-sulfonylamino derivatives of minocycline have been synthesized for structure–activity relationship studies. These compounds showed activity against both tetracycline-susceptible and tetracycline-resistant strains. Many of the 9-sulfonylamino derivatives exhibited improved antibacterial activity against a number of tetracycline- and minocycline-resistant Gram-positive pathogens.

Graphical abstractNovel sulfonamide and acylamino derivatives of minocycline were synthesized. Many of these derivatives exhibited potent antibacterial activity against tetracycline- and minocycline-resistant Gram-positive pathogens.Figure optionsDownload full-size imageDownload as PowerPoint slide