We studied the effects of an analogue of isonicotinic acid hydrazide on the treatment course of experimental tuberculosis. Complex analysis has demonstrated the efficiency of isonicotinic acid hydrazide immobilized on a carrier that consisted of water-soluble cation-active analogue of chitosan (N-chlorohydroxypropyl chitosan) in a complex with cobalt ions in the therapy of experimental tuberculosis. Immunostimulating activity of the polymeric metal complex was revealed. The obtained data can be used for the development of highly effective methods for tuberculosis treatment.
No abstract
Synthesis of Monosaccharides of Unsaturated Esters.-Methacryloyl-O-glycosides are prepared starting from D-glucosides or Dmannosides via diboronate glycosides, selective hydrolysis to give diboronates, acylation with methacryloyl anhydride, and final removal of boronate groups by methanolysis to give esters like (VI). Acryloyl ester (X), 3-acryloyl-D-glucose, and 1-acryloyl-L-sorbose are obtained by another route involving the acylation of diisopropylidene protected sugars with acryloyl chloride and subsequent removal of the isopropylidene groups by treatment with formic acid or in the presence of KU-2-8 catalyst.-(SLIVKIN, A. I.; LAPENKO, V. L.; Izv.
As is known, some water-soluble polyelectrolytes (glycans, nucleic acids, synthetic polycarboxylic acids and their copolymers with pyridine derivatives, etc.) exhibit adjuvant properties when introduced into the organism together with antigens [1]. However, most of the synthetic polyelectrolytes exhibit increased toxicity, which is an obstacle for their use in immunolo~cal research [2]. A promising way to the creation of low-toxicity polymers possessing immunomodulator properties consists in the chemical modification of glycans that are characterized by detoxicating effect and are capable of prolonging and au.~aenting the action of drugs used for chemotherapy. Smirnova et al. [3] reported on the synthesis of an oxyglycan based on mannan, a microbial poIysaccharide capable of stimulating the immune response [3].The purpose of this work was to synthesize nontoxic water-soluble polymers (analogs of oxystarch and inulin), containing amino acid and hydroxyalkyl(alkyl)amino groups and study their biolo~cal activity.The oxystarch was obtained through the oxidation of starch by the persulfate method, whereby 12% aldehyde and 8% carboxy groups (occupying predominantly the C o and C 3 positions) are formed in the structure [4].The starch-based cation-active derivatives were synthesized by interaction of oxyglycan with (3-chloro-2-hydroxypropyl)tri(2-hydroxyethyl)ammonium chloride or triethylamine with the formation of ethers and salts (I and II, respectively). The carionization of inulin was performed by, its interaction with di(2-hydroxyethyl)amine and formaldehyde (the Marmieh reaction). The resulting amino-containing ethers are probably substituted at the C 6 site (V). The results of periodate oxidation indicate that OH groups in positions C 3 and C 4 (a-glycol group) are free (as is known, some structtaaI features of inulin hinder substitution of these hydroxy groups) [5,6]. 80,c3/H~H OH Starch analogs of the ampholytic type were obtained by the reaction of oxystarch with N-0aydroxymethyl)-L-gluramie acid (leading to the formation of iminium-salt structural elements with an aldehyde group conversion from 3 to 12%, IVa-IVc) and lysine (with the formation of azomethine group, liD. Compounds I-V were synthesized in an aqueous medium at a temperature of 50-70~ The structures of polymer analogs were confirmed by IR spectroscopic data and the results of elemental analyses. EXPERIMENTAL CHEMICAL PARTThe IR spectra of synthesized compounds were measured on an IKS-29 spectrophotomcter.Compounds I -V were purified by ultrafiltmtion through fluoroplastic membranes with a pore diameter of 50 A for compound V and 200 A for compounds I -IV.
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