Synthesis, in vitro, and in vivo antibacterial activity of nocathiacin I thiol-Michael adducts

The synthesis and antibacterial activity of a series of nocathiacin I derivatives (4–20) containing polar water solubilizing groups is described. Thiol-Michael adducts containing acidic polar groups have reduced antibacterial activity whereas those with basic polar groups have retained very good antibacterial activity.

Graphical abstractThe synthesis and antibacterial activity of nocathiacin I analogues is described.Figure optionsDownload full-size imageDownload as PowerPoint slide