Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones

• Published in: Bioorganic & medicinal chemistry letters 2007-09, Vol.17 (18), p.5227-5232
• Main Authors: Srivastava, Brijesh Kumar, Soni, Rina, Patel, Jayendra Z., Solanki, Manish, Valani, Darshan, Gupta, Sunil, Mishra, Bhupendra, Takale, Vijay, Pandya, Purvi, Jain, Mukul R., Patel, Pankaj R.
• Format: Article
• Language: English
• Subjects: Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Antibacterial agents; Antibiotics. Antiinfectious agents. Antiparasitic agents; Biological and medical sciences; Gram-positive organism; In vitro MIC assay; Linezolid resistant Staphylococcus aureus; Medical sciences; Microbial Sensitivity Tests; N-Methylamino piperidinylaryloxazolidinones; Oxazolidinones - chemical synthesis; Oxazolidinones - chemistry; Oxazolidinones - pharmacology; Pharmacology. Drug treatments; Piperidines - chemistry
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2007.06.075

Design and synthesis of a few novel methylamino piperidinyl substituted oxazolidinones are reported and their antibacterial activities have been evaluated in MIC assay against broader panel of both susceptible and resistant Gram-positive strains. Design and synthesis of a few novel methylamino piperidinyl substituted oxazolidinones are reported. Their antibacterial activities have been evaluated in a MIC assay against broader panel of both susceptible and resistant Gram-positive strains. ( S)- N-{3-[3-Fluoro-4-(methyl-{1-[3-(5-nitrofuran-2-yl)-acryloyl]-piperidin-4-yl}-amino)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide 4i has shown comparable antibacterial activity to linezolid and eperezolid in the MIC assay, additionally compound 4i showed good antibacterial activity with an in vitro MIC value of 2–4 μg/mL against linezolid resistant Staphylococcus aureus (linezolid ⩾16 μg/mL).