Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents.
A series of 4-arylpiperazin-1-yl-3-phenyloxazolidin-2-one derivatives with diversification of the N-substituents such as methylene O-linked heterocycles, thioamide, dithiocarbamate, thiourea, and thiocarbamate were synthesized and evaluated as antibacterial agents. Their in vitro activities (MIC) were evaluated against MRSA and VRE resistant Gram-positive strains such as Staphylococcus and Enterococcus. Most of the compounds were more potent in vitro but less active in vivo than linezolid.
Jang
Sun-Young
SY
Imagene Co. Ltd, Biotechnology Incubating Center, Seoul National University, Seoul 151-742, South Korea.
Ha
Young Hwan
YH
Ko
Seung Whan
SW
Lee
Wonku
W
Lee
Jongkook
J
Kim
Sunghoon
S
Kim
Yong Woo
YW
Lee
Won Koo
WK
Ha
Hyun-Joon
HJ
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013293:Enterococcus faecalis / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D010879:Piperazines