Design, synthesis and biological evaluation of paralleled Aza resveratrol–chalcone compounds as potential anti-inflammatory agents for the treatment of acute lung injury

Acute lung injury (ALI) is a major cause of acute respiratory failure in critically-ill patients. It has been reported that both resveratrol and chalcone derivatives could ameliorate lung injury induced by inflammation. A series of paralleled Aza resveratrol–chalcone compounds (5a–5m, 6a–6i) were designed, synthesized and screened for anti-inflammatory activity. A majority showed potent inhibition on the IL-6 and TNF-α expression-stimulated by LPS in macrophages, of which compound 6b is the most potent analog by inhibition of LPS-induced IL-6 release in a dose-dependent manner. Moreover, 6b exhibited protection against LPS-induced acute lung injury in vivo. These results offer further insight into the use of Aza resveratrol–chalcone compounds for the treatment of inflammatory diseases, and the use of compound 6b as a lead compound for the development of anti-ALI agents.

Paralleled Aza resveratrol–chalcone compounds were synthesized and evaluated for anti-inflammatory activities in the treatment of ALI.Figure optionsDownload as PowerPoint slide