Novel 4-N-substituted aryl but-3-ene-1,2-dione derivatives of piperazinyloxazolidinones as antibacterial agents.
Novel (5S)-N-[3-(3-fluoro-4-{4-[2-oxo-4-(substituted aryl)-but-3-enoyl]-piperazin-1-yl}-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide 3a-j analogues were synthesized and their in vitro antibacterial activity was evaluated. Most of the compounds of series showed superior in vitro activity against Gram-positive resistant strains than linezolid. Compound 3f is the most potent compound in the series with 0.04-0.39 microg/mL MIC.
Varshney
Vandana
V
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India.
Mishra
Nripendra N
NN
Shukla
Praveen K
PK
Sahu
Devi P
DP
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002073:Butanes / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D002073:Butanes; D023303:Oxazolidinones