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Synthesis and Biological Activity Research of Rimantadine Schiff Bases

Author: WangDongJing
Tutor: LiuBin
School: Liaoning University
Course: Medicinal Chemistry
Keywords: Schiff bases rimantadine antibiotic interaction bovine serum albumin(BSA) DNA
CLC: R914
Type: Master's thesis
Year: 2012
Downloads: 42
Quote: 0
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Abstract


Schiff bases are a category of compounds containing C=N group. It is reportedthat many schiff bases show a variety of interesting biological actions, includingantibacterial, antifungal, and anticancer actions. So, in recent years, some researcheshave been concentrated on the synthesis and biological investigation of schiff bases.Protein and DNA are the basic composition of all organisms and play an importantrole in life processes. Investigation of the interaction between small molecules andbiomacromolecule is helpful for us to understand the mechanism of drugs, explain themetabolism process and provide the evidence of course genetic. In this paper, wesynthesized five rimantadine schiff bases (RSBs) and investigated the biologicalactivity of them. The major contents of this paper are as follows:Firstly, five RSBs were synthesized by the condensation reaction of rimantadinewith salicylaldehyde and its derivatives under anhydrous conditions, respectively.The structure of compounds were characterized by infrared spectroscopy,1H NMR,simultaneously, the melting points of the compounds were measured.Secondly, the inhibitory effect on E. coli and Staphylococcus aureus of RSBswas investigated by plate diffusion method. The study found that RSBs showeddifferent degrees of inhibition against both bacterium and the antibacterial activityagainst E. coli was stronger than that of Staphylococcus aureus. Schiff basessynthesized by rimantadine and5-substituted salicylaldehyde derivatives showedantibacterial effect against E. coli better than the other schiff bases.Thirdly, bovine serum albumin (BSA) as a target protein, the interaction ofRSBs and BSA was studied using UV spectroscopy, fluorescence spectroscopy,synchronous fluorescence spectra, and circular dichroism spectroscopy. The resultsshowed that fluorescence of BSA was quenched remarkably by these compounds, thequenching mechanism was static quenching and nonradiative energy transfer. Bindingstrength of compounds and BSA was in the following order:RNS>RMS>RS>ROV>RCS. The receptor sites of RSBs on the BSA were Site I.Interaction of RSBs and BSA made a change in the conformation of BSA, the hydrophobicity of the tryptophan residues microenvironment changed.Lastly, the interaction between the RSBs and calf thymus DNA was studied byultraviolet spectroscopy, fluorescence spectroscopy, viscosity combining. The resultsfound that the mode of action between the RSBs with DNA was groove combination.Fluorescence spectroscopy experiments showed that the RSBs combined with theDNA-BR system to form the DNA-BR-RSBs complexes, thereby quenching thefluorescence of DNA-BR system.

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