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.
Biochemicals Research Center, Korea Institute of Science and Technology, Cheongryang, Seoul 130-650, South Korea.
Jae Seok
JS
Lee
Yong Seo
YS
Cho
Moon Ho
MH
Chang
Hun Yeong
HY
Koh
Bong Young
BY
Chung
Ae Nim
AN
Pae
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