[Synthesis and in vitro antibacterial activities of new 3,5-disubstituted oxazolidinone compounds].
OBJECTIVE
To design and synthesize new oxazolidinone antibacterial agents.


METHODS
The synthetic method reported in literature has been modified and new 3,5-disubstituted oxazolidinone compounds were synthesized on the basis of SAR reported in the literature and their antibacterial activities in vitro were determined.


RESULTS
Eighteen new objective compounds were synthesized, and their structures were determined by IR, 1HNMR and FAB-MS. Within the eighteen new objective compounds, sixteen compounds showed antibacterial activity in vitro and compound 9, 10 and 10b showed better antibacterial activities in vitro than ciprofloxacin (CIP), sultamicillin (Sul) and vancomycin (VCO). Compounds 9a and 11c have no antibacterial activity in vitro at all.


CONCLUSIONS
Compounds 9, 10 and 10b are worthy to be intensively studied.
Meng
Qing-guo
QG
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China. qinggmeng@yahoo.com.cn
Wang
Qi
Q
Liu
Jun
J
D000667:Ampicillin / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002939:Ciprofloxacin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013291:Streptococcus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013407:Sulbactam / Q000494:pharmacology; D014640:Vancomycin / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D002939:Ciprofloxacin; C035444:sultamicillin; D014640:Vancomycin; D000667:Ampicillin; D013407:Sulbactam