| Immune drugs developed in the1970s, are a newly rising class of therapeutic drugs,which depends on the multi-disciplinary research foundation of the tumor chemotherapy, theorgan transplanting, the immune pathology and the clinical immunology and so on.FTY-720was synthesized by Professor Fujita in1995with Yoshitomi PharmaceuticalCompany and become a brandnew immunosuppressant. The chemical name is called2-amino-2-[2-(4-octyl-phenyl) ethyl]-1,3-propanediol hydrochloride. It was synthesized bymodificationg the structure of ISP-1, which is a sphingosine-like substance separating fromculture medium of Chinese Cordyceps. In2010, FTY-720has been approved by FDA as afirst-line treatment drug for multiple sclerosis.In this paper, the present situation as well as the immunosuppressant of FTY-720features and other aspects of the comprehensive are summaried. Based on our research fornew immunosuppressive agents FC in our laboratory, we have designed and synthesized aseries of amino alcohols derivatives, and inhibition of lymphocyte activity was tested.We have already understood the immunosuppressive status and the characteristic aswell as structure-activity relationship of FTY-720. Based on our research for newimmunosuppressive agents FC in the laboratory, we have designed and synthesized a seriesof7-substituted,2-tetralone as the starting material, then KCN addition, hydrolysis,reduction to give the aim compounds-FC-042.We used chemical method for separating the enantiomers of FC-042, and obtained twocompound the (+) FC-042and (-) FC-042. Meanwhile, the inhibition of mouse lymphocyteactivity was tested. Pharmacological experiments showed that amino alcohols derivativeshave an inhibitory effect on lymphocytes.The QSAR study found that: the based structure of the compound is tetralin, the2position was substituted by hydroxymethyl and amino; the7position was substituted by(benzyloxy) phenylthio have activity effectively. |
