Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties

• Published in: Bioorganic & medicinal chemistry letters Vol. 18; no. 21; pp. 5815 - 5818
• Main Authors: Kim, Seoung Jong, Jung, Myung-Ho, Yoo, Kyung Ho, Cho, Jung-Hyuck, Oh, Chang-Hyun
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 01.11.2008; Elsevier
• Subjects: Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - pharmacology; Antibacterial activity; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Biological and medical sciences; Cyclic sulfonamide; Gram-Negative Bacteria - drug effects; Gram-Positive Bacteria - drug effects; Medical sciences; Microbial Sensitivity Tests; Oxazolidinones; Oxazolidinones - chemical synthesis; Oxazolidinones - pharmacology; Pharmacology. Drug treatments; Sulfonamides - chemistry; Cyclic sulfonamide; Oxazolidinones; Antibacterial activity; Enterococcus; Sulfonamide; Vancomycin; In vitro; Biological activity; Haemophilus influenzae; Meticillin; Pasteurellaceae; Resistance; Streptococcaceae; Streptococcus; Sulfonamides; Oxazolidinone derivative; Bacteria; Micrococcales; Micrococcaceae; Fluorine Organic compounds; Antibacterial agent; Chemical synthesis; Staphylococcus aureus
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2008.09.034

The synthesis of a new series of oxazolidinones having cyclic sulfonamide moieties is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituents on the oxazolidinone ring was investigated. A particular compound 15g having [1,2,5]thiadiazolidin-1,1-dioxide moiety showed the most potent antibacterial activity. The synthesis of a new series of oxazolidinones having cyclic sulfonamide moieties is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituents on the oxazolidinone ring was investigated. A particular compound 15g having [1,2,5]thiadiazolidin-1,1-dioxide moiety showed the most potent antibacterial activity.