Synthesis And Characterization Of Amino Acid Conjugates Of Piperazine, Pentacyclic Triterpenoids And Uracil Compounds, And The Study On The Biological Activity

Amino acids are collectively of a class of organic compounds containing amino group and carboxyl group, and it is a basic structure unit of organism protein, enzymes and other biological macromolecules. It can be divided into protein amino acid and non-protein amino acid two categories. Many amino acids is not only nutrients of the body, but also has a certain therapeutic effect on some diseases. It shows a variety of biological activity such as antitumor, anti-inflammatory, antiviral, hypoglycemic and many other kinds of pharmacological effects.Amino acid is an essential nutrient of the body. Introduction of amino acid on the lead compounds has a synergistic effect and can improve its water-solubility, the capability of target location and bioavailability to a certain extent.This dissertation adopts the splice theory used in drug, guided by organic chemical theory, combined the achievements of biological activity test. Some biological compounds and amino acid are spliced together in order to obtain drugs of better biological activity.In this dissertation, the research work can be divided into three parts:Firstly, we mainly describe the biological activity of piperazine, oleanolic acid, ursolic acid, fluorouracil and thymine, respectively, and give a brief introduction of amino acid and amino-protecting groups.Secondly, by exploring the synthesis, separation and purification conditions,20kinds of amino acid conjugates were designed and synthesized. Specifically to do the work as follows:(1). The four amino acids which amino group was protected were introduced into N-1and N-4position of the piperazine, and then removing the protecting group, eight amino acids conjugates were synthesized. The conjugates were characterized by IR and1H NMR.(2). Eight derivatives of pentacyclic triterpenoids were synthesized through modification at C-28of oleanolic acid and ursolic acid, and introducing amino acid at C-3position. The conjugates were characterized by IR、1H NMR and13CNMR.(3). The research introduced two carbon linkage at N-1position of fluorouracil and thymine, followed by introducing amino acid at glycol to form four amino acids derivatives. The conjugates were characterized by IR and1H NMR.Thirdly, The amino acid conjugates of piperazine were studied by the antibacterial activity. The amino acid conjugates of pentacyclic triterpenoids and uracils were studied by the antitumor activity.