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Information × Registration Number 0299U004392, 0197U000423 , R & D reports Title Obtaining of new biological active compounds on a basis of muramyldipeptide and natural triterpenoids. popup.stage_title Head Chyrva Vasyl' Yakovych, Registration Date 07-06-2001 Organization National Taurida V. Vernadsky University popup.description2 Object of research are derivatives of N-acetylmuramyl-L-alanyl-D-isoglutamine (MDP) and natural triterpenoids. The purpose of research is development of methods of synthesis of new biologically active compounds - analogues of glycopeptides of bacterial cell. Search, allocation and establishment of structure new triterpenoids from plants Araliaceae family, having immunoadjuvant properties. Synthesis of conjugates of muramylpeptides and triterpenoids with the purpose of reception of the compounds having raised, in comparison with initial components, immunoactivity. The research will be carried out with attraction of modern methods of organic chemistry, chemistry of carbohydrate and peptides. The structure of the synthesized and allocated preparations is established with the help of spectral and chemical-analytical methods. For confirmation of a conclusion about of a configuration of anomeric centre and biological activity of muramylpeptides, and also for study of influence of an aglycon nature on biologi cal effect the synthesis several anomeric pairs of glycosides of MDP was undertaken. The features of biological properties of these compounds testify to validity of the made earlier assumptions. The synthesis of disaccharide-octapeptide structurally similar to oligomeric fragment of bacterial peptidoglycan is carried out. Unlike of natural analogue sythetic oligomer has fixed b- configuration of anomeric centre, that should result in additional increase of its biological activity. The methods of obtaining of pure triterpene alcohol - methyl ether of oleanolic acid from the sum Calendula medicinal is developed. The method of glycosilation triterpene glycosides of low reactivity triterpene alcohols is developed and key the derivative - b-D-N-acetylglucosaminide of methyl ether of oleanolic acid is received. It has developed new more effective syntheses of others key intermediates: aliphatic and aromatic glycosides of N-acetyl-D-glucosamine and benzyl ester of Boc-L-alanyl-D-isoglutamine which are necessary for economic obtaining of preparative quantities of glycopeptides. With the purpose of search of new sources biologically active natural triterpenoids is investigated glycosidic structure of three kinds of ivy - Hedera helix L., Hedera canariensis Willd. and Hedera colchica C.Koch. More of 50 individual pure glycosides of oleanolic and echinocystic acids, hederagenin, 30-norhederagenin and caulophillogenin were isolated. A number of received glycosides is new chemical compounds/ for the majority of isolated triterpene glycosides immunoactivity in relation to fibers of a virus HIV-1 is established and investigated, and also the influence of saponins on reproduction of a human immunodeficiency virus in vitro is revealed. The melting points are determined on the device PTP. The optical rotation was measured with the Polamat-A polarimeter. 1H-NMR spectra are received on the Bruker WP-200 (200 МГц), Varian Geminy-200 (200 МГц), Varian VXR-300 (300 МГц) and Bruker WМ-500 (500 Мгц) spectrometers. TLC on the Kieselgel 60 -F254 (Merck) and Silufol UV-254 (Kavalier) plates. КХ on the Aldrich 70 - 230 mesh, Merck 240 - 400 mesh and L-40/100 (Lachema) gel. The received substances can be used in research institutes and organizations engaged in questions of immunology, creation of vaccines, and also development of methods of preventive maintenance of diseases of an agricultural animal. Product Description popup.authors popup.nrat_date 2020-04-02 Close