The new hypolipidemic natural active substances Adipostatin A and Its Derivatives
|School||Shenyang Pharmaceutical University|
|Keywords||Hyperlipemia The blood-lipid lowering drag Adipostain A 3-Phosphoglycerate dehydrogenase Synthesis|
The advance of the blood-lipid lowering drug was reviewed in the paper; the structure and activity of resorcinolic lipids and the mechanism of new blood-lipid lowering active compound Adipostatin A was also introduced.The synthetic route of Adipostatin A were studied and total yield of seven steps amounted to 35.2%, the structure was eluvidate through physic-chemica lproperties and spectroscopic analyses. The preparation of the key intermediates was investigated; the improved methods were developed for the prearation of the key intermediates methyl 3,5-dimethoxybenzoate, 3,5-dimethoxybenzaldehyde, n-C14H29Br. The synthetic method was simplified and improved.In addition, the structure—activity relationships of Adipostatin A and resorcinolic lipids were summed up. Based upon it, 20 compounds were designed and synthesized, 15 have not been reported in literature. The structure was eluvidate through physic-chemical properties and spectroscopic analyses.The improved methods were developed for the prearation of the analoguses—1-hydroxy-3-methoxy-5-pentadecylbenzene. Compared with the method in the literature, this new method was simplified and improved.The enzyme inhibition in vitro and the activity of blood-lipid lowering in vivo are studying.