Design And Synthesis Of Derivatives Of γ-DDB And Study On Their Qsar

4,4'-Dimethoxy-5.6,5',6'-bis(memylenedioxy)-2,2'-dimethoxy carbonyl biphenyl ( Y -DDB). which was discovered in the process of studying the anti-hepatotoxic components from Schizandra chinensis, has been well known as an effective agent for liver protect. It has a high biologic activity though its' poor bioavailability and is deserving for research as a lead compound. It can decrease hepatic damage and hepatocytes necrosis induced by chemical substance such as carbon tetrachloride, D-galactosamin or thioacetamide, lower the level of serum glutamic-pyrumic transaminase(GPT) and glutamic-oxalacetic transaminase (GOT), relieve the symptom of intoxicant hepatitis caused by chemotherapy agents such as Fluorouracil, Methotrexate. r-DDB has no mutagenicity or malformationity and low toxicity. But without acting on virus, about half of the patients has the effect of "back up" after stopping the administration of the drug .This curriculum design to add a medicine or a radical which has anti-virus activity with the Y -DDB , and through these medicines' "Firstpass effect" in hepatic , we hope to inhibit or remove the hepatic virus utterly when its' lowe'r the level of GPT ,so may improve its' anti virus activity on hepatic.In this curriculum we synthesized 13 derivatives of f-DDB, 12 of them were new compounds. Their structures were confirmed by 1H-NMR and MS. The pharmacological test showed that some of these compounds could lower the level of serum GPT .