Discovery and synthesis of novel substituted benzocoumarins as orally active lipid modulating agents

The synthesis of a series of benzocoumarin keto-enamine schiff bases is reported. The novel compounds were evaluated for their antihyperlipidemic activity in the hyperlipidemic hamster model. The compound 11 at a dose of 10 mg/kg body weight significantly lowered the plasma triglyceride levels (TG) by 70%, total cholesterol (TC) by 47%, accompanied by an increase in HDL-C/TC ratio by 80% in hyperlipidemic hamsters to a greater degree than the reference drugs atorvastatin and lovastatin.

Figure optionsDownload as PowerPoint slideHighlights
► Synthesis and antidyslipidemic activity of novel benzocoumarins is reported.
► Compound 11 showed better activity than the reference drugs in HFD fed hamsters.
► Dose response studies revealed 25 mg/kg as most optimum dose.