Synthesis and antibacterial activities of eperezolid analogs with glycinyl substitutions.
A series of eperezolid analogs with glycinyl substitutions were prepared and their antibacterial activities were studied against a panel of susceptible and resistant Gram-positive bacteria. The compounds with N-arylacyl or N-heteroarylacyl glycinyl structural units showed good antibacterial activities. The compounds 11b, 11c, and 11e were twofold more active than linezolid against Staphylococcus epidermidis and Enterococcus faecalis. Several pyridine analogs were also prepared and found to have poor antibacterial activity against most of the tested Gram-positive bacteria, however, one of the compounds 12e showed very high activity against Enterococcus faecalis.
Wang
Xiao-Jun
XJ
Industrial Institute of Fine Chemicals and Synthetic Drugs, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, P.R. China.
Wu
Ning
N
Du
Guang-Jian
GJ
Zhao
Shuang-Qi
SQ
Yan
Ming
M
Gu
Lian-Quan
LQ
D000081:Acetamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013293:Enterococcus faecalis / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D000069349:Linezolid; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013212:Staphylococcus epidermidis / Q000187:drug effects; D055672:Static Electricity
D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; C098011:eperezolid; D000069349:Linezolid