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Synthesis, Structure And Biological Evaluation Of Transition Metal Complexes With Cinnamate Derivates And Organic Diamines

Posted on:2015-10-13Degree:MasterType:Thesis
Country:ChinaCandidate:H ZhuFull Text:PDF
GTID:2284330431979330Subject:Biophysics
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Cinnamic acid, a derivative of phenylalanine, is a kind of organic acid. Aderivative of cinnamic acid shown the potential antibacterial, antifungal, antitumour,antitubercular and antioxidant activities. In the pharmaceutical industry the derivativeof cinnamic acid are widely used in anti-tumor therapy and other diseases. Transitionmetals were required because of some of their biologically activity for manybiochemical processes. Some of them acted as cofactor in some of important enzymesresulte in increasing the activities of these enzymes, even can cure some diseasesdirectly. But they cannot take direct absorption and even cause toxicity. Peoplesupposed that the functional activity would be optimized by combining transitionmetals with organic acids and the adverse reaction would be avoided at the same time.In recent years, many novel transition metal complexes were described, the biologicalactivity of transition metal complexes was the focus of scientists’ attention and hadbeen reported many times. Especially the potent inhibitory activity against bacteriaand tumor.New ligands of cinnamic acid derivatives were synthesized in this paper. Fivenew transition metals complexes with organic amine had been synthesized andcharacterized by X-ray single crystal determination and the FT-IR. We evaluationedthe inhibitory activity on jack bean urease and the antimicrobial activities selectivly.(1) The veratraldehyde was chosen to prepare a new kind of cinnamic acidderivative by the method of chemical synthesize:(E)-3-(3,4-dimethoxyphenyl)acrylic acid. The method of conventional solution reaction was used to synthesizethree new kinds of metal complexes: The transition metal complex of(E)-3-(3,4-dimethoxyphenyl) acrylic acid, Cu(II) and1,2-propanediamine (transitionmetal complex1); The transition metal complex of (E)-3-(3,4-dimethoxyphenyl)acrylic acid, Cu(II) and1,3-propanediamine (transition metal complex2); Thetransition metal complex of (E)-3-(3,4-dimethoxyphenyl)acrylic acid, Ni(II) andethanediamine (transition metal complex3). The inhibitory activity on jack bean urease shows that the whole three new metal complexes have the ability to restrainthe activity of urease. It was found that copper(II) complexes1[IC50=4.71μM] and2[IC50=3.15μM] showed strong inhibitory activity against jack bean urease, comparedwith the ligand (E)-3-(3,4-dimethoxyphenyl) acrylic acid.(2) The p-(Methyl-sulfonyl)benzaldehyde was chosen to prepare a new kind ofcinnamic acid,(E)-3-(4-(methylsulfonyl)phenyl) acrylic acid. The method ofconventional solution reaction was put to use to synthesize two new kinds of Zn(Ⅱ)transition metal complexes: The transition metal complex of (E)-3-(4-(methylsulfonyl)phenyl)acrylic acid, Zn(Ⅱ),4,4’-bipyridine (transition metal complex4); Thetransition metal complex of (E)-3-(4-(methylsulfonyl)phenyl)acrylic acid, Zn(Ⅱ),3-((1H-imidazol-1-yl)methyl)pyridine (transition metal complex5). The test, whichshows that the whole metal complexes of Zn(Ⅱ) have the antimicrobial activities butunsatisfactory.
Keywords/Search Tags:Cinnamic acid, Transition metal complex, Crystal structures, Ureaseinhibitors, Antimicrobial activities
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