title: Novel Oxazolidinone Antibacterial Analogues with a Substituted Ligustrazine C-ring Unit.
abstract: 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.
authors: College of Pharmacy, Jinan University, Guangzhou, 510632, China.
authors: Yan
authors: Y
authors: Chen
authors: College of Pharmacy, Jinan University, Guangzhou, 510632, China.
authors: Zhi-Xiong
authors: ZX
authors: Ruan
authors: College of Pharmacy, Jinan University, Guangzhou, 510632, China.
authors: Fang
authors: F
authors: Wang
authors: College of Pharmacy, Jinan University, Guangzhou, 510632, China.
authors: De-Sheng
authors: DS
authors: Huangfu
authors: College of Pharmacy, Jinan University, Guangzhou, 510632, China.
authors: Ping-Hua
authors: PH
authors: Sun
authors: College of Pharmacy, Jinan University, Guangzhou, 510632, China.
authors: Jing
authors: J
authors: Lin
authors: College of Pharmacy, Jinan University, Guangzhou, 510632, China.
authors: Wei-Min
authors: WM
authors: Chen
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line / Q000187:drug effects / Q000378:metabolism; D060326:Chemistry Techniques, Synthetic; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006094:Gram-Positive Bacteria / Q000187:drug effects; D015850:Interleukin-6 / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests; D009569:Nitric Oxide / Q000378:metabolism; D023303:Oxazolidinones / Q000737:chemistry*; D011719:Pyrazines / Q000737:chemistry; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000378:metabolism; D000093242:Interleukin-6 Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D015850:Interleukin-6; D008070:Lipopolysaccharides; D009569:Nitric Oxide; D023303:Oxazolidinones; D011719:Pyrazines; D014409:Tumor Necrosis Factor-alpha; D000093242:Interleukin-6 Inhibitors; C577686:interleukin-6, mouse; C017953:tetramethylpyrazine
keywords: anti-inflammatory; antibacterial; ligustrazine; linezolid; oxazolidinone