Novel Oxazolidinone Antibacterial Analogues with a Substituted Ligustrazine C-ring Unit

作者：Chen, Yan; Ruan, Zhi Xiong; Wang, Fang; Huangfu, De Sheng; Sun, Ping Hua; Lin, Jing; Chen, Wei Min^*

来源：Chemical Biology & Drug Design, 2015, 86(4): 682-690.

DOI：10.1111/cbdd.12537

• antibacterial
• anti-inflammatory
• ligustrazine
• linezolid
• oxazolidinone

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.

• 出版日期2015-10
• 单位暨南大学