Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with 4 H -pyran-4-one and pyridin-4-one substitution in the C-14 side chain

A series of novel pleuromutilin derivatives with 4H-pyran-4-one and pyridin-4-one substitution in the C-14 side chain have been synthesized. Structure–activity relationship study showed that 4H-pyran-4-one moiety is favored over pyridin-4-one. Among the series, compounds 12a, 12d and 28 exhibited excellent antibacterial activity against selected Gram-positive strains including MRSA, MRSE, and PRSP.