ZHAI Xin, ZHANG Guo-gang, GOU Dong-hui, LIU Jun-peng, GONG Ping. Modification of novel oxazolidinone derivatives at C-5 side chain and their antibacterial activitiesJ. Acta Pharmaceutica Sinica, 2006, 41(10): 985-989.
Citation: ZHAI Xin, ZHANG Guo-gang, GOU Dong-hui, LIU Jun-peng, GONG Ping. Modification of novel oxazolidinone derivatives at C-5 side chain and their antibacterial activitiesJ. Acta Pharmaceutica Sinica, 2006, 41(10): 985-989.

Modification of novel oxazolidinone derivatives at C-5 side chain and their antibacterial activities

  • AimTo modify the C-5 side chains of the oxazolidinone derivatives and evaluate their in vitro antibacterial activities preliminarily. MethodsThe 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. ResultsThirty 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. ConclusionCompounds 7a, 9a and 11a were worth further studying.
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