Synthesis Of 1-erucic Acyl-4-benzyl Piprazine Derivatives And Research On Vivo & Vitro Pharmacological Activity Thereof

Background Alzheimer's disease,a sort of nervous-systematically retrogressive disease,the patho-mechanism of which is not yet very clear,is supposed to occur with Free radical Injuries and Inflammatory Reactions as its possible inductions.With further and deeper studies going on, medications thereof tend to be multi-target effects oriented,and those being free-radical scavengers,antioxidants and antiphlogistons,show various potential advantages.AIM Lead compound-erucic acid shows its pharmacological actions in free-radical scavenging property,antioxidation and antiphlogosis.With possible reconstitutions on different situs,a series of 1-erucic acyl-4-benzyl piprazine derivatives were designed and synthesized,followed by vivo and vitro pharmacological experiments,with an expectation to find out some new molecules to be more therapeutically effective,specifically selective and,less side-effective.ExperimentalSynthesis A series of 1-sinapic acyl-4-benzyl piprazine derivatives were synthesized via Knoevenagel Condensation Reaction,phenolic hydroxyl group acetylation, halogen-displacement reaction on carboxy-hydroxy,N-nomo-alkylation,N- acetylation and ester alcoholysis.Pharmacology Pharmacological activities,lying in hydroxy free-radical scavenging property,DPPH free-radical scavenging property and anti-inflammatory effect,were determined via Ferrosin-Fe 2+ Oxidation Method,DPPH-Static Force Method and Swelling of mouse ear Method respectively.ResultOn synthesis A series of 1-erucic acyl-4-benzyl piprazine derivatives were successfully synthesized with identifications in EA,MS,1H-NMR and IR.On pharmacology 1.Comparison between Hydroxy Radical Scavenging Activity Properties1 SA3,SA4,SA5,SA6,SA7 and SA9,3-CH3,2-CH3,4-OCH3,3-OCH3,2-OCH3 and 3-Cl benzyl-benzene-ring-substitutes of FA respectively,all exhibit Emax-values higher than FA and VC(positive controls).2 SA6 and SA10,3-OCH3 and 2-Cl benzyl-benzene-ring-substitutes of FA respectively, exhibit IC50 values lower than VC,to suggest...