Zemlyakov O. Muramylpeptides: synthesis and biological activity

Object of investigation: muramylpeptides, glycosides of N-acetylglucosamine, conjugates. Aim of investigation: elaboration of effective modification of muramyldipeptide; synthesis of perspective for use in immunology and medicine new analogues of MDP; establishment of structural factors, affecting biological activity derivatives of MDP. Methods of investigation and instruments: organic synthesis, IR-, NMR-spectroscopy. Theoretical results and novelty: new derivatives of mono- and disaccharidedipeptides and conjugates of MDP are sinthesized. The synthesis of a- and b-N-acetylglucosaminides in presence mercury(II) iodide as catalysts by Koenigs-Knorr reactions are studied. High effectiveness of b-О-glycosidations of muramyldipeptide and lowering of biological activity by a-О-glycosidations were established. Practical results and novelty: The new synthesis of key intermediates - glycosides of N-acetylglucosamine and dipeptides, are elaborated. The "instruments" for study of mechanisms of glycopeptide biol ogical actions (polyacrylamide probes and 14C-labelled muramylpeptides) and glycopeptide, which can be used as immunostimulators and adjuvants, are sinthesized. Subject and degree of introduction: patent, application of present work results in scientific and education practice in universities and institutes of Ukraine; permission on use b-heptylglycosides of MDP as biologically active food additions is got. Efficiency of inculcation caused due to the more perfect synthesis methods derivative of MDP and more active muramyldipeptides. Field of application: chemistry, medicine.