Syntheses and biological evaluation of phosphoryl-containing polyunsaturated fatty acid derivatives as hypolipidemic agents

GRAPHICAL ABSTRACT

ABSTRACT

A series of novel compounds phosphoryl-containing polyunsaturated fatty acid derivatives n-(diisopropoxy-phosphonamide)-alkyl ester (2a–2o) have been synthesized and evaluated for lowering hypolipidemia activities. Amongst all the synthesized compounds, compound 2d, 2h, and 2m showed significant lowering of triglyceride (TG) by 47.37%, 45.88%, and 45.69%, respectively, in triton induced hyperlipidemic in mice. Furthermore, compound 2d showed potent antihyperlipidemic activity and was found to decrease the plasma total cholesterol levels (TC) by 53.3%, TG by 29.3%, in high-fat diet induced hyperlipidemic in mice.

KEYWORDS:

• Syntheses
• polyunsaturated fatty acid
• lowering hypolipidemia activities

Funding

The authors would like to acknowledge the Science and technology planning project of Fujian Province (Grant no. 2014Y0068). The work was supported by Fujian Collaborative Innovation Center for Exploitation and Utilization of Marine Biological Resources, the Third Institute of Oceanography of the State Oceanic Administration, Xiamen, Fujian, P.R. China.