[Modification of novel oxazolidinone derivatives at C-5 side chain and their antibacterial activities].
OBJECTIVE
To modify the C-5 side chains of the oxazolidinone derivatives and evaluate their in vitro antibacterial activities preliminarily.


METHODS
The title compounds were synthesized in 9 - 12 steps with the starting material 3-fluoroaniline and their in vitro antibacterial activities were examined by using Mueller-Hinton broth dilution method.


RESULTS
Thirty new compounds were designed and synthesized, in which eighteen novel title compounds were prepared and their structures were confirmed by 1H NMR and ESI-MS. Eleven compounds showed antibacterial activities to a certain extent, among them compounds 7a, 9a and 11a displayed promising activity.


CONCLUSIONS
Compounds 7a, 9a and 11a were worth further studying.
Zhai
Xin
X
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.
Zhang
Guo-Gang
GG
Gou
Dong-Hui
DH
Liu
Jun-Peng
JP
Gong
Ping
P
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones