N-thiolated 2-oxazolidinones: A new family of antibacterial agents for methicillin-resistant Staphylococcus aureus and Bacillus anthracis

• Published in: Bioorganic & medicinal chemistry letters Vol. 16; no. 8; pp. 2081 - 2083
• Main Authors: Mishra, Rajesh Kumar, Revell, Kevin D., Coates, Cristina M., Turos, Edward, Dickey, Sonja, Lim, Daniel V.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 15.04.2006; Elsevier
• Subjects: Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - pharmacology; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Bacillus anthracis; Bacillus anthracis - drug effects; beta-Lactams - pharmacology; Biological and medical sciences; Drug Resistance, Microbial; Medical sciences; Methicillin Resistance; Microbial Sensitivity Tests; MRSA; N-thiolated 2-oxazolidinones; N-thiolated β-lactam; Oxazolidinones - chemical synthesis; Oxazolidinones - pharmacology; Pharmacology. Drug treatments; Staphylococcus aureus; Staphylococcus aureus - drug effects; Sulfhydryl Compounds - chemistry; Bacillus anthracis; N-thiolated β-lactam; N-thiolated 2-oxazolidinones; MRSA; Bacillaceae; In vitro; Biological activity; Meticillin; Resistance; Bacillales; Oxazolidinone derivative; Bacteria; Micrococcales; Micrococcaceae; Antibacterial agent; Chemical synthesis; Staphylococcus aureus
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2006.01.058

A new family of N-thiolated 2-oxazolidinones having antibacterial activity against methicillin-resistant Staphylococcus aureus and Bacillus anthracis is reported. The effect of ring substituents and stereochemistry on antibacterial activity of these compounds was found to be similar to that of previously reported N-thiolated β-lactams. In this report, we describe a new family of N-thiolated 2-oxazolidinones having antibacterial activity against methicillin-resistant Staphylococcus aureus and Bacillus anthracis. The effect of ring substituents and stereochemistry on antibacterial activity of these oxazolidinones closely parallels that previously reported for N-thiolated β-lactam antibiotics.