Study On The Design And Synthesis Of Artemisinin-nucleoside Conjugates As Virus Inhibitors

Acquired immune deficiency syndrome (AIDS) and type B viral hepatitis, which were caused by human immunodeficiency viruses (HIV) and hepatitis B viruses (HBV) respectively, are two types of severe infective diseases which seriously threaten the health of human being. HIV can attack the cell immune system in human body, destroy T4 Lymphocytes, weaken the resistance of organism, ruin the immune system, and eventually cause many opportunistic infections and tumors to make people death. HBV, with strong communicability, is a type of viruses which can infect hepatic cells and induce inflammation and necrosis. Heretofore, there are no good therapies to cure both two diseases. Thus, developing new potent anti-virus drugs is very important and become the main ways to cure AIDS and type B viral hepatitis.Artemisinin derivatives contain unique structure of peroxide bridge and have special mechanisms of anti-malaria and anti-tumor activity. A lot of reports present that besides their anti-malaria and anti-tumor activity, artemisinin derivatives had anti-virus activity against HIV, hepatitis virus, cytomegalovirus, coxsackie b virus, and so on.Based on principle of prodrug and hybridization, the lead compound dihydroartemisinine were linked to anti-virus drugs of nucleosides to form conjugates via different type of binary acids by twice of esterification. Sixteen compounds were synthesized and not been report in literature. Linking the compound with undestroyed active group to another may produce a more potent anti-virus drug. This conjugate may be led to action targets, acts as a multi-target and multi-effect anti-virus drug, makes synergistic effect and improves its anti-virus activity significantly. The structures of target compounds were confirmed by 1H-NMR, FAB-MS and elemental analysis.The anti-HIV and anti-HBV activity of target compounds will be assayed.