Synthesis,Structure Modification And Biological Evaluation Of Bornoel Derivatives

Stroke is a common disease which causes serious danmage to human health and life safety.Stroke pose great threat to health and life of mankind and bring about agony for patient,also serious burden for families and societies.So it’s time to realize thoroughly the severity of stroke,advancing standards of treatments and prophylaxis of stroke,Decreasing the incidence,mutilation rate,mortality of it.In recent years,many natural compounds are reported,with its new mechanisms,high specificity,moderate function and the little adverse effect,which arouse high interests all over the world.As a traditional chinese medicine,borneol can be used for treating stroke,coma,faint,carbuncle and hot eyes duo to its fuctions of inducing resuscitation,clearing heat and alleviating pain.Borneol is usually used as medicinal usher or adjuvar.It is widely used for treating Cardiocerebral vascular Diseases as a component of compatibility of drugs in Chinese patent drug.All these experimental results above indicate that borneol could improve neurological deficits,protect damaged neuron caused by cerebral ischemia and its mechanisms maybe related to inhibiting the action of lipid peroxidation by cutting down contents of MDA,increasing activities of SOD,LDH,GSH-Px and Injury of inflammation,restraining the platelet aggregation,resisting thrombopoiesis,adjusting energy metabolism,et al.Therefore,borneol is a good lead compound to design anti-cerebral ischemia drugs.In this dissertation,borneol is the lead compound.The structure modification was performed on three aspects:1.The structure modification was performed on 2-OH of bomeol;2.The structure modification was performed on 1-NH2 of 2,6-Diisopropylaniline;3.The structure modification was performed on 2-OH of menthol.There is a hope that borneol derivatives which have better pharmacological activity can be found through these studies to get anti-cerebral ischemia drugs with independent intellectual property rights.Structure and activity relationship is summarized to lay a solid base for searching for new type of medicines which have novel mechanism of action,reliable curable effect and low toxic effects for treatment of stoke and other disease.