The Design And Synthesis Of Chemicals For The Treatment Of Alzheimer's Disease

Alzheimer's disease(AD).It is a disease that progressively degrades with age.AD can be diagnosed with a combination of questionnaire scores and brain mri.The causes of alzheimer's disease are related to various factors,including environmental factors,genetic factors,age factors,gender factors,and self.The mechanism of pathogenesis is also unclear,there are many hypothesis theories,and it is generally accepted that the amyloid protein hypothesis.A variety of pathogenesis of alzheimer's disease have a variety of clinical symptoms:memory loss,blurred vision,grumpy,depression and could cause some infections.The more advanced the AD is,the greater the harm,not only the health of the patient,but also the family.Therefore,early diagnosis and early treatment is important,but because the pathogenesis is not clear,so far AD cannot be completely cured.Through the study of different pathogenesis and different hypothesis theories,people also began to explore and study the drugs of corresponding mechanism.At present,the natural products used to treat alzheimer's disease are huperzine,clausenamide,schisandra,saponins and so on.chemical synthesis or semi-synthetic drugs include galanthamine,donepezil,rivastigmine,tacrine and so on.At present,its have many drug researches on the treatment of AD,the?-secretase enzymes modulator the target is also popular.A large number of relevant studies have been reviewed,we found that the Phenylmidazole is a good active functional group.with phenylimidazole as the unchanging skeleton,and the modification of its polysubstitution can produce a series of compounds.In this paper,A and B series of compounds were synthesized by using imidazole as the invariable structure.The compound A series was synthesized by the reaction of phenyl-imidazolamide and 4 bromophenylac-etic anhydride to produce pentamethyl cyclic amide,and have synthesis of 25 new compounds by the Suzuki coupling reaction with various substituted phenylboronic acid.The compound B series was synthesized by three steps.first,The dehydrogenation of benzoindolic acid and the polysubstituted aniline in the protection of BOC,second,Remove the BOC protection group.third,Condensation with phenylmidazole acid.finally,10 new compounds were obtained.The new drug molecular structures of A series and B series are characterized by~1H NMR and carbon spectra and high resolution mass spectra.The biological activity data of two series of compounds are in preparation for testing.