Pleuromutilin derivatives having a purine ring. Part 2: Influence of the central spacer on the antibacterial activity against Gram-positive pathogens

Structural modification of the 4-piperidinethio moiety, as a spacer of the first pleuromutilin analogues 2A and 2B having a purine ring, led to discovery of the novel pleuromutilin derivatives 14B and 17B. These compounds with good solubility in water showed promising in vitro antibacterial activity against various Gram-positive bacteria including MRSA, PRSP, and VRE and have potent in vivo efficacy.

Graphical abstractStructural modification of the 4-piperidinethio moiety, as a central spacer of the pleuromutilin analogues 2A and 2B with excellent in vitro and in vivo antibacterial activities and good solubility in water, led to the discovery of the novel and promising compounds 14B and 17B.Figure optionsDownload full-size imageDownload as PowerPoint slide