Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
A series of isoxazolyl tetrahydropyridinyl oxazolidinones with various substituents at the 3-position of the isoxazole ring have been synthesized and their in vitro antibacterial activities (MIC) were evaluated against several Gram-positive strains including the resistant strains of Staphyloccus and Enterococcus, such as MRSA and VRE. One of the most potent compounds synthesized, 4f, showed comparable or better activity against selected bacterial strains than those of linezolid and vancomycin.
Lee
Jae Seok
JS
Biochemicals Research Center, Korea Institute of Science and Technology, Cheongryang, Seoul 130-650, South Korea.
Cho
Yong Seo
YS
Chang
Moon Ho
MH
Koh
Hun Yeong
HY
Chung
Bong Young
BY
Pae
Ae Nim
AN
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016983:Enterococcus / Q000187:drug effects / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013210:Staphylococcus / Q000187:drug effects / Q000254:growth & development; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones