Pleuromutilin derivatives having a purine ring. Part 1: New compounds with promising antibacterial activity against resistant Gram-positive pathogens

In the course of our research aimed at the discovery of metabolic stable pleuromutilin derivatives with more potent antibacterial activity against Gram-positive pathogens than previous analogues, a series of compounds bearing a purine ring were prepared and evaluated. From SAR studies, we identified two promising compounds 85 and 87, which have excellent in vitro activity against a number of Gram-positive pathogens, including existing drug-resistant strains, and potent in vivo efficacy.

Graphical abstractIn the course of our research aimed at the discovery of the metabolically stable pleuromutilin analogues with potent antibacterial activity against Gram-positive pathogens, we have found two promising compounds, bearing a purine ring and having potential as novel antibacterial agents for use in human.Figure optionsDownload full-size imageDownload as PowerPoint slide