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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
chemistry
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones
European Journal of Medicinal Chemistry, Volume 44, No. 8, Year 2009
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Description
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. © 2009 Elsevier Masson SAS. All rights reserved.
Authors & Co-Authors
Phillips, Oludotun Adebayo
Kuwait, Kuwait City
Kuwait University
Udo, Edet Ekpenyong
Kuwait, Kuwait City
Kuwait University
Abdel-Hamid, Mohammed E.
Kuwait, Kuwait City
Kuwait University
Varghese, Reny
Kuwait, Kuwait City
Kuwait University
Statistics
Citations: 78
Authors: 4
Affiliations: 1
Identifiers
Doi:
10.1016/j.ejmech.2009.03.024
ISSN:
02235234
e-ISSN:
17683254