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Novel Oxazolidinone Antibacterial Analogues with a Substituted Ligustrazine C‐ring Unit
Author(s) -
Chen Yan,
Ruan ZhiXiong,
Wang Fang,
Huangfu DeSheng,
Sun PingHua,
Lin Jing,
Chen WeiMin
Publication year - 2015
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/cbdd.12537
Subject(s) - linezolid , chemistry , nitric oxide , antibacterial activity , in vitro , tumor necrosis factor alpha , ring (chemistry) , stereochemistry , combinatorial chemistry , anti inflammatory , pharmacology , biochemistry , bacteria , staphylococcus aureus , organic chemistry , biology , immunology , vancomycin , genetics
A series of novel oxazolidinone compounds with a substituted ligustrazine C‐ring unit and different substituted groups at the C‐5 side chain were designed and synthesized using linezolid as a lead and based on a scaffold hopping strategy. Their antibacterial and anti‐inflammatory activities were evaluated. The results of in vitro antibacterial assays showed that all fourteen target compounds displayed potent activity against Gram‐positive pathogens, particularly 8b , 13b , 14a , 14b , 15a, and 15b . Moreover, 14a and 14b exhibited significant inhibitory activities on the production of inflammatory mediators, including nitric oxide, interleukin‐6, and tumor necrosis factor‐alpha. Thus, these derivatives could serve as valuable candidates to develop anti‐infective agents for the treatment of chronic wounds.