We identified a series of 2-phenyl-ethenesulfonic acid phenyl ester analogues as novel dual-function agents that suppressed nitric oxide production in lipopolysaccharide/interferon γ-stimulated RAW264.7 cells and activated peroxisome proliferator-activated receptor γ (PPARγ) in a cell-based transactivation assay. Western blot analysis demonstrated that these compounds inhibit the expression of inducible nitric oxide synthase protein, and scintillation proximity assay validated their ability to bind to PPARγ. Our studies provide the basis for developing these dual-function agents for anti-inflammation and anti-atherosclerosis therapy. ? 2008 Elsevier Ltd. All rights reserved.
Date:
2008-10-15
Relation:
Bioorganic and Medicinal Chemistry Letters. 2008 Oct 15;18(20):5676-5679.
