The fi rst description of oxazolidinones as antibacterials was reported by researchers from the DuPont company in 1987. Compounds Dup-105 and DuP-721 (Fig. 1) were introduced as clinical candidates with good activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus, in an in vivo animal effi cacy model (1). These compounds demonstrated lethal toxicity in animal models and were not further developed (2). Researchers at Pharmacia (now Pfi zer) became interested in these molecules and began a chemistry/screening effort to improve the in vitro, in vivo, and safety profi les of oxazolidinones.
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Shinabarger, D., Eliopoulos, G.M. (2009). Resistance to Linezolid. In: Mayers, D.L. (eds) Antimicrobial Drug Resistance. Infectious Disease. Humana Press. https://doi.org/10.1007/978-1-59745-180-2_22
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