Synthesis of new andrographolide derivatives and evaluation of their antidyslipidemic, LDL-oxidation and antioxidant activity

•Fifteen derivatives of andrographolide prepared.•All the compounds were screened for their antidyslipidemia, LDL-oxidation and antioxidant activity.•One of the derivatives 7 turned out be more potent than the parent compound and comparable to marketed drugs.

Andrographis paniculata, native to Taiwan, Mainland China and India, is a medicinal herb, which possesses various biological activities including anti-atherosclerosis. Andrographolide (1) has been identified as one of the active constituents against atherosclerosis. In continuation of our drug discovery program we synthesized few novel derivatives of 1 to improve their antidyslipidemic, LDL-oxidation and antioxidant activity. The tosylated derivative 7 has been turned out to be more potent than the parent compound and comparable activity with marketed antidyslipidemic drugs.

Graphical abstractFew new derivatives of andrographolide (1) were synthesized and evaluated their antidyslipidemic, LDL oxidation and antioxidant activity. The tosylated derivative 7 has comparable activity to the marketed antidyslipidemic drugs.Figure optionsDownload full-size imageDownload as PowerPoint slide