Synthesis and in vitro antibacterial activities of new 3,5-disubstituted oxazolidinone compounds.
- Author:
Qing-guo MENG
1
;
Qi WANG
;
Jun LIU
Author Information
- Publication Type:Journal Article
- MeSH: Ampicillin; pharmacology; Anti-Bacterial Agents; chemical synthesis; chemistry; pharmacology; Ciprofloxacin; pharmacology; Microbial Sensitivity Tests; Molecular Structure; Oxazolidinones; chemical synthesis; chemistry; pharmacology; Staphylococcus aureus; drug effects; Streptococcus; drug effects; Structure-Activity Relationship; Sulbactam; pharmacology; Vancomycin; pharmacology
- From: Acta Pharmaceutica Sinica 2003;38(10):754-759
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo design and synthesize new oxazolidinone antibacterial agents.
METHODSThe 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.
RESULTSEighteen 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.
CONCLUSIONCompounds 9, 10 and 10b are worthy to be intensively studied.
