Synthesis and antibacterial activity of C-2(S)-substituted pleuromutilin derivatives

In order to probe the effect of C-2(S)-substituted groups in the antibacterial activity, a series of novel C-2(S)-substituted pleuromutilin analogues of SB-225586 were synthesized and evaluated for their in vitro antibacterial activity. The results of antibacterial activities indicated that C-2(S)-substituted pleuromutilin derivatives retained appreciable antibacterial activity, and the 2-fluorination compounds 6a and 6b are more potent than the corresponding 2-hydroxylation analogues 7a and 7b.