Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
We have prepared and evaluated the antibacterial activities of a series of substituted methylenepiperidinyl and methylenepyrrolidinyl oxazolidinones against several gram-positive strains including the resistant strains of Staphyloccus and Enterococcus, such as MRSA, CRSA, MSSA and VRE. Some of them showed comparable or superior in vitro activities (MIC) to vancomycin.
Kim
Hye Yeon
HY
Biochemicals Research Center, Korea Institute of Science and Technology, Cheongryang, 130-650, Seoul, South Korea. hykoh@kist.re.kr
Lee
Jae Seok
JS
Cha
Joo Hwan
JH
Pae
Ae Nim
AN
Cho
Yong Seo
YS
Chang
Moon Ho
MH
Koh
Hun Yeong
HY
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D019540:Area Under Curve; D001419:Bacteria / Q000187:drug effects*; D024881:Drug Resistance, Bacterial; D016983:Enterococcus / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007202:Indicators and Reagents; D008297:Male; D008826:Microbial Sensitivity Tests; D010080:Oxazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship; D014640:Vancomycin / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D007202:Indicators and Reagents; D010080:Oxazoles; D010880:Piperidines; D011759:Pyrrolidines; C482000:methylenepiperidinyl oxazolidinone; C481999:methylenepyrrolidinyl oxazolidinone; D014640:Vancomycin