Research paperDesign of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites

Add time:08/22/2019    Source:sciencedirect.com

The aim of this study was to design and synthesize COX-1/COX-2 balanced inhibitors incorporating the structural motifs of anti-inflammatory ascidian metabolites. We designed a series of substituted indole analogs that incorporate the key structures of the ascidian metabolites, herdmanines C and D. The synthesized analogs were tested for their inhibitory activity against COX-1 and COX-2, and compound 5m, which displayed balanced inhibition, was further evaluated for in vitro anti-inflammatory activity. Compound 5m suppressed the expression of pro-inflammatory factors, including iNOS, COX-2, TNF-α, and IL-6 in LPS-stimulated murine RAW264.7 macrophages. The reduction of PGE2, NO, and ROS was also observed, together with the suppression of NF-κB, IKK, and IκBα phosphorylation. Our results characterized 5m as a COX-1/COX-2 balanced inhibitor that subsequently caused ROS inhibition and NF-κB suppression, and culminated in the suppression of iNOS, COX-2, TNF-α, and IL-6 expression.

We also recommend Trading Suppliers and Manufacturers of 3-AMINO-1H-INDOLE-2-CARBOHYDRAZIDE (cas 110963-29-6). Pls Click Website Link as below: cas 110963-29-6 suppliers

Prev:Chapter 4 - Synthesis of Other Isocoumarin Derivatives
Next:Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system)