Abstract
ABSTRACT Four novel pleuromutilin derivatives with butyl amine group in the C-14 side-chain were designed, synthesized and confirmed by FT-IR, 1 H-NMR and HR-MS. The results of antibacterial activity showed that the antibacterial activity of pleuromutilin derivatives could be affected by the steric hindrance of their C-14 side-chain. Key words: pleuromutilin derivatives, antibacterial, Staphylococcus aureus . INTRODUCTION Due to the dramatic increasing of antibiotic resistance among pathogenic bacterial strains, research efforts are focusing on new antibiotics that have unique modes of action and activity against resistant organisms. During the past 25 years, the number of antibiotics which have been approved by the Food and Drug Administration (FDA) decreased annually. 1 Actually, after the discovery of sulphonamide antibiotics in the 1930s and penicillin in the 1940s, there were only three novel classes of antibacterials, the topical antibiotic mupirocin, the oxazolidinones (linezolid) and the cyclic lipopeptides (daptomycin) which had entered the market.
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