Synthesis and biological evaluation of novel thiazolidinone derivatives as potential anti-inflammatory agents.

TitleSynthesis and biological evaluation of novel thiazolidinone derivatives as potential anti-inflammatory agents.
Publication TypeJournal Article
Year of Publication2013
AuthorsHu J, Wang Y, Wei X, Wu X, Chen G, Cao G, Shen X, Zhang X, Tang Q, Liang G, Li X
JournalEuropean journal of medicinal chemistry
Volume64
Pagination292-301
Date Published2013 Jun
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.

DOI10.1038/nm.3162
Alternate JournalEur J Med Chem