High hypolipidemic activity of saturated side-chain alpha-asarone analogs

With the aim of evaluating the pharmacophore potential of the side chain of alpha -asarone (1) regarding its high hypolipidemic activity, the series o f derivatives 7a-7e, and 11-13 were evaluated pharmacologically. For the hy drocarbon compounds 7a-7e, with a variable-size side chain, significant dec reases in serum cholesterol, LDL-cholesterol, and triglyceride levels and s ignificant increases in HDL-cholesterol levels were observed in mice. The s mall-size side-chain derivatives were even more active than 1 in reducing c holesterol. The results suggested that the length and saturated character o f the side chain seem to be a key feature in improving hypolipidemic activi ty of alpha -asarone (1) analogs.