Design And Synthesis Of Isoflavones And Their Derivatives

Nonsteroidal anti-inflammatory drug (NSAIDs) which not only used in the treatment of rheumatoid arthritis, osteo arthritis, other arthritis, some diseases associated with arthritis and pain, but also used in the preservation of colon cancer and Alzhemimer’s Disease(AD) etc, are widely used in many countries. However, most of NSAIDs used in clinic now tend to induce gastrointestinal damage, nephrotoxicity and hepatotoxicity. Therefore, the discovery of novel anti-inflammatory with high anti-inflammatory effects and low toxicities has become an important research field.Isoflavonoids are a family of naturally compounds which are abundant in plant kingdom. These natural compounds as potential therapeutic agents have been of interest to the medicinal chemists for many years because of their broad biological activities such as antitumour, antioxidant, antiallergic and anti-inflammatory etc.Because some isoflavonoids and oxazine derivatives exhibit good anti-inflammatory activities reported in literatures, and some compounds such as 1,3-benzoxazine derivatives of 4-chromanones, 4-chromones exhibit anti-inflammatory activities are found in our laboratory, in order to discover new anti-inflammatory agents, based on the principles of hybridization and bioisosterism, eight of 1,3-benzoxazine derivatives with isoflavone scaffold, and six of 7-(4-alkolaminoalkoxy)-3-phenyl-4H-benzopyran-4-one derivatives were designed, synthesied, and characterized by proton NMR, EI-MS and IR in this thesis. All target compounds are the novel compounds which are not reported in the literature based on search by SciFinder and other database.The anti-inflammatory activities for fourteen target compounds are under studying.