Design of Agents Interacting with Immunoregulating Proteins:Potential Inhibitors of the Phenylpyruvate Tautomerase Activity Catalysed by Macrophage Migration Inhibitory Factor (MIF)  

作　　者：CARPY Alain J.M. HAASBROEK P.P. OLIVER D.W. 

机构地区：[1]PTC-UMR 5472 CNRS,Department of Pharmacy and Pharmacology,Pharmacology Faculty of Health Science University of Bordeaux I,Talence, France ,University of Witwatersrand, Johannesburg,South Africa,Potchefstroom University for CHE, Potchefstroom,South Africa

出　　处：《Chinese Journal of Chemistry》2003年第10期1256-1262,共7页中国化学（英文版）

基　　金：ProjectsupportedbytheFrenchGovernmentandtheNationalResearchFoundationinSouthAfrica

摘　　要：The macrophage migration inhibitory factor has been implicated in a number ofimmune and inflammatory processes. MIF presents particular opportunities for drug design anddevelopment with potential therapeutic applications. Drug design strategies taking intoconsideration of specific stereochemical and tautomeric requirements in the interaction of MIF withsubstrates and inhibitors allow several novel structures to be designed. Our investigationssuccessfully explored the tautomeric and stereochemical aspects of new compounds of the2-phenylpyruvic acid type, both experimentally, through synthesis and structural investigations andcomputationally, through molecular mechanics and quantum mechanics calculations.The macrophage migration inhibitory factor has been implicated in a number ofimmune and inflammatory processes. MIF presents particular opportunities for drug design anddevelopment with potential therapeutic applications. Drug design strategies taking intoconsideration of specific stereochemical and tautomeric requirements in the interaction of MIF withsubstrates and inhibitors allow several novel structures to be designed. Our investigationssuccessfully explored the tautomeric and stereochemical aspects of new compounds of the2-phenylpyruvic acid type, both experimentally, through synthesis and structural investigations andcomputationally, through molecular mechanics and quantum mechanics calculations.

关 键 词：macrophage migration inhibitory factor phenylpyru-vate tautomerase activity AZLACTONE phenylpyruvic acid derivative 

分 类 号：TQ463[化学工程—制药化工]