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Synthesis and Antibacterial Activity of a Series of α‐Substituted Acetylpiperazinyl Oxazolidinones
Author(s) -
Wang XiaoJun,
Du GuangJian,
Zhao ShuangQi,
Yan Ming,
Gu LianQuan
Publication year - 2009
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2009.00859.x
Subject(s) - linezolid , enterococcus faecalis , staphylococcus epidermidis , staphylococcus aureus , antibacterial activity , chemistry , microbiology and biotechnology , gram , bacteria , biology , vancomycin , genetics
A series of oxazolidinone derivatives with α‐substituted acetylpiperazinyl groups were prepared. Their in vitro antibacterial activities were studied against Gram‐positive pathogens, including methicillin‐resistant Staphylococcus aureus , Staphylococcus aureus , Staphylococcus epidermidis and Enterococcus faecalis . The compounds with chloroacetyl‐piperazinyl or dichloroacetyl‐piperazinyl group were found to have superior antibacterial activities to linezolid against most of tested Gram‐positive pathogens. The compounds with propionylpiperaziny or fluoroacetylpiperazinyl group were found to have comparable antibacterial activities with linezolid. However, the replacement of phenyl ring of the compounds with pyridine ring resulted in the significant loss of antibacterial activity.