期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 8, 页码 3217-3227出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.03.024
关键词
Antibacterial; Linezolid; Monoamine oxidase; PH-027; 5-(4-Methyl-1,2,3-triazole)methyl oxazolidinone; Oxazolidinone
资金
- Research Administration, Kuwait University [PC01/05]
- [GS01/01]
- [GS03/01]
A series of 5-(4-methyl-1,2,3-triazole)methyl oxazolidinones were synthesized and tested for their antibacterial activity against a panel of Gram-positive and Gram-negative clinical isolates in comparison with linezolid and vancomycin. Most of the compounds demonstrated strong to moderate in vitro antibacterial activity against susceptible and resistant Gram-positive pathogenic bacteria. Antibacterial activity varied with substitutions at the phenyl C4 position with bulky alkylcarbonyl and alkoxycarbonyl substitutions on the piperazine N4 being detrimental to antibacterial activity. Whereas the presence of the 4-methyl-1,2,3-triazole moiety in the acyl-piperazine containing analogs resulted in increased protein binding, and decreased antibacterial activity particularly against Streptococcus pneumoniae strains. (C) 2009 Elsevier Masson SAS. All rights reserved.
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