title: Synthesis and biological evaluation of novel thiazolidinone derivatives as potential anti-inflammatory agents.
abstract: The modulation of pro-inflammatory cytokines provides a target for controlling inflammatory diseases and attracts much attention in current anti-inflammatory drug development. Here, four series of thiazolidinone derivatives were synthesized and screened for anti-inflammatory activities. A majority of these compounds showed excellent inhibition on the expression of TNF-α and IL-6 in LPS-stimulated macrophages. Discussions are given regarding the structure-activity relationships. Compounds 12d and 12h inhibited LPS-induced TNF-α and IL-6 release in a dose-dependent manner. Furthermore, 12d exhibited a significant protection against LPS-induced septic death in mouse model. Together, these data present a series of new thiazolidinones with potential therapeutic effects in acute inflammatory diseases and they could be important leads in the continuing anti-inflammatory drug research.
authors: School of Pharmaceutical Sciences, Wenzhou Medical College, University Town, Chashan High-Education Park, Wenzhou, Zhejiang 325035, China.
authors: Jie
authors: J
authors: Hu
authors: Yi
authors: Y
authors: Wang
authors: Xiaoyan
authors: X
authors: Wei
authors: Xixi
authors: X
authors: Wu
authors: Gaozhi
authors: G
authors: Chen
authors: Gaozhong
authors: G
authors: Cao
authors: Xueqian
authors: X
authors: Shen
authors: Xiuhua
authors: X
authors: Zhang
authors: Qinqin
authors: Q
authors: Tang
authors: Guang
authors: G
authors: Liang
authors: Xiaokun
authors: X
authors: Li
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015850:Interleukin-6 / Q000096:biosynthesis; D008070:Lipopolysaccharides / Q000008:administration & dosage / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D015996:Survival Rate; D053778:Thiazolidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D000093242:Interleukin-6 Inhibitors
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D015850:Interleukin-6; D008070:Lipopolysaccharides; D053778:Thiazolidines; D014409:Tumor Necrosis Factor-alpha; D000093242:Interleukin-6 Inhibitors