5-hydroxy-6-methyl-1-(thietanyl-3)pyrimidine-2,4(1h,3h)-dione, inhibiting generation of active forms of oxygen

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound - 5-hydroxy-6-methyl-1-(thietanyl-3)pyrimidine-2,4(1H,3H)-dione of formula , which inhibits generation of active forms of oxygen and has antioxidant activity.

EFFECT: improved properties of compounds.

2 cl, 1 dwg, 1 tbl, 2 ex

 

The present invention relates to organic chemistry and medicine, in particular to a new connection - 5-hydroxy-6-methyl-1-(titanyl-3)pyrimidine-2,4(1H,3H)-dione, the vast generation of reactive oxygen species (ROS) and a potent antioxidant.

Known substance with antioxidant activity, which refers to pharmaceutically acceptable salts of 2,4,6-trimethyl-3-hydroxypyridine with lower dicarboxylic acids [patent RU 2276138, 2006].

You know the tool that represents 5-amino-6-methyluracil, which exhibits antioxidant activity [patent RU 2398767, 2010].

Known application of sulfate 2-phenyl-3-(3,4-acid)-4-(2-morpholinoethyl)pyrrolo[1,2-a]benzimidazole as a means with antiradical activity, cerebroprotective and anti-ischemic properties [patent RU 2445090, 2012].

As a prototype, and the comparison drug taken methyluracil (6-methylpyrimidin-2,4(1H,3H)-dione), used in medical practice [Mashkovsky PPM Medicines. // M LLC "New wave", 2004 - Vol.2, p.160-161], antioxidant activity which is described in [Shishkin, L.N., Taran P., Eliseev S.V., Bulgakov V.G. Influence of 6-methyluracil oxidative reactions in model systems of different complexity. "Izv. Academy of Sciences, ser. Biol., 1992. No. 3. - s-357; Yakupov LR,Ivanov A.V., Safiullin R.L., Gimadieva A.R., Chernyshenko, Y., Mustafin A.G., Abdrakhmanov IB // Inhibitory effect of derivatives of 6-methyluracil on free radical oxidation of 1,4-dioxane, Izv. Academy of Sciences, ser. chem., 2010, No. 3, s-511].

The objective of the invention is to expand the Arsenal of biologically active compounds, including potent antioxidant.

The technical result - obtaining biologically active substance that suppresses the generation of reactive oxygen species and possessing antioxidant activity.

The essence of the invention: 5-hydroxy-6-methyl-1-(titanyl-3)pyrimidine-2,4(1H,3H)-dione of the formula (I):

suppressing the generation of reactive oxygen species.

The specified connection and its properties are not described in literature.

The inventive compound is synthesized by alkylation of 5-hydroxy-6-methylpyrimidin-2,4(1H,3H)-dione 2-chloromethylstyrene in the presence of potassium hydroxide in the aquatic environment.

Example 1

The synthesis of the claimed compounds.

To a solution of 1.34 g (24 mmol) of potassium hydroxide in 20 ml of water is added 2,84 g (20 mmol) 5-hydroxy-6-methylpyrimidin-2,4(1H,3H)-dione and heated to 50°C. Then add 2.3 g (22 mmol) of 2-chloromethylstyrene and stirred for 2 hours at 50-55°C. the Precipitate is filtered from the hot reaction mixture is treated with ethyl acetate, hot water, dried at 60°C. TPL=204-206°C. On ucaut 1.12 g (26%) of 5-hydroxy-6-methyl-1-(titanyl-3)pyrimidine-2,4(1H,3H)-dione, purify by crystallization from an ethanol water mixture (volume ratio 1:1). Neproreagirovavshimi 5-hydroxy-6-methylpyrimidin-2,4(1H,3H)-dione quantitatively return in the synthesis.

IR spectrum, ν, cm-1: 703 (S(CH2)2), 1239 (C-N), 1724 (C2=O), 1650 (C4=O), 1629 (C=C), 2807-3192 (N-H, O-H).

An NMR spectrum1N (DMCO-d6), δ, ppm: 2.02 (3H, s, 6-CH3); 3.10-3.16 (2H, m, S(CH)2); 3.37-3.43 (2H, m, S(CH)2); 4.80-4.91 (1H, m, NCH); 10.45 (1H, ush. C, 3-NH).

An NMR spectrum13(DMCO-d6), δ, ppm: 13.26 (6-CH3); 35.69 (NCH); 74.32 (S(CH2)2); 127.65 (C-5); 142.44 (C-6); 149.89 (C-2); 160.61 (C-4).

Elemental analysis.

Found, %: C 44.74; N, 4.75; N, 13.12 - C8H10N2O3S.

Calculated, %: C at 44.85; N, 4.70; N, 13.07.

The inventive compound is a white to yellowish or pinkish tinge crystalline powder, insoluble in water, ethanol, chloroform, soluble in dimethylformamide, dimethylsulfoxide, alkali solutions.

Example 2

Evaluation of the effect of the inventive compounds on the generation of ROS.

The effect of the claimed compounds and drug comparisons on the processes of free radical oxidation in model systems in vitro was studied using a rapid method for determination of antioxidant activity based on detection of chemiluminescence (CHL) fluorescence arising from the interaction of free radicals (Baimatov V.N., Headlight is urdinov P.P., Bagautdinov A.M. // Chemiluminescent methods for the study of free radical oxidation in agriculture, veterinary medicine and animal husbandry. - Ufa, Izd-vo "Health of Bashkortostan", 2009. - 104 S.).

The chemiluminescence was detected on the installation HLM-003 (Russia). Chlorophyll model systems were characterized by spontaneous light emission, quick flash and then developing a slow flash. The main most informative characteristics of CHL serve sutasoma glow determined by the intensity of the radiation, and the maximum amplitude of the glow.

To assess the impact on the processes of SRO in vitro studies were performed on model systems that generate ROS.

As a model system, where the generated ROS, used 10 ml of phosphate buffer (20 mm KH2PO4, 105 mm KCl) with the addition of a solution lyuminola (10-5M) and sodium citrate (50 mm). The pH of the resulting solution was brought to 7.45% by titration with a saturated solution of caustic potash. To initiate the reactions, accompanied by the formation of ROS, was introduced 1 ml of 50 mm solution of salts of Fe2+. Check the glow lasted for 5 minutes with constant stirring.

The drugs were added in the model system in concentrations not exceeding therapeutic dose of the drug methyluracil used in medical PR is ctice. As control was used a model system in which instead of the investigated drugs were added to 0.9% saline in the same volume.

The invention is illustrated in the figure, which presents the effect of the claimed compounds and methyluracil on the processes SRO in the model system of active forms of oxygen, where: K - control, I - the claimed compound II - drug comparison methyluracil.

As a result of researches it is established that the claimed compound reduces spontaneous luminescence and a quick flash, surpassing drug comparison (figure). Inhibition of PI depended on the concentration of the drug (0.01 mg/ml; 0.1 mg/ml; 1.0 mg/ml) (table). Than it was greater, was suppressed glow, this is evidence of communication holdem from free radical oxidation.

Presents the chemical compound inhibits the generation of active forms of oxygen, at a concentration of 1.0 mg/ml surpassing methyluracil 3.5 times, which indicates the presence of the antioxidant properties of the claimed compounds.

1. 5-hydroxy-6-methyl-1-(titanyl-3)pyrimidine-2,4(1H,3H)-dione of the formula

2. The substance according to claim 1, the vast generation of reactive oxygen species.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to an improved method for preparing 2-arylamino-4-hetarylpyrimidines of formula (I) which possess inhibitory action on serine-threonine kinase Haspin on the enzymatic level, and may be used as drug substances for oncological diseases. In formula (I), wherein Het = , , , , , , , , , , ,

R=H; 2-Me; 3-Me; 4-Me; 2,3-di-Me; 2-MeO; 3-MeO; 4-MeO; 4-EtO; 4-PhO; 2-Cl; 3-Cl; 4-Cl; 4-F; 2-Me, 3-Cl. The method consists in a reaction of related hetarylmethylketone and N,N-dimethylformamide dimethylacetale on boiling of reagents in isopropyl alchohol for 6 hours to produce 3-dimethylamino-1-hetaryl-2-propen-1-ones with adding in situ related aryl guanidine and further boiling for 2 hours. The process is conducted at molar ratio (mole) of hetarylmethylketone: N,N-dimethylformamide dimethylacetale : aryl guanidine = 1:1.5:1.

EFFECT: method simplifies the process due to cutting a process time and reducing consumption of the initial ingredients.

6 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to a novel compound - 6-methyl-1-(thietanyl-3)uracil of formula 1 , which stimulates the protective activity of phagocytes.

EFFECT: obtaining compounds which stimulate the protective activity of phagocytes.

2 cl, 1 dwg, 1 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to organic chemistry and medicine and specifically to a novel compound - 6-(thietanyl-3)aminopyrimidine-2,4(1H,3H)-dione of formula (1), which inhibits lipid peroxidation.

EFFECT: obtaining a compound which inhibits lipid peroxidation.

2 cl, 1 dwg, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cyclic indole-3-carboxamide of formula (I) or physiologically acceptable salts thereof of formula (I): wherein the values A, R, R10, R20, R30, R40, n, p and q are specified in clause 1 of the patent claim. A method for preparing them is described.

EFFECT: compounds have renin-inhibitory activity that allows using them for preparing a pharmaceutical composition and a drug preparation for treating the diseases associated with renin activity.

11 cl, 4 tbl, 127 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formulae

,

where X is O, NH or N-Rx, and Rx, Ra, Rb, R10a, R11a, R2, R3, R4 are selected from hydrogen, different aliphatic, alicyclic, aromatic, heteroaromatic and functional groups which can be optionally substituted, wherein R4 together with R2 can form a C1-C5alkylene or C3-C5alkenylene fragment. Said compounds are positive modulators of metabotropic glutamate receptor 2 and can be used in medicine.

EFFECT: novel biologically active compounds are efficient when treating a range of diseases of the nervous system which are mediated by the dysfunction of the glutamate receptor.

23 cl, 590 ex, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to organic synthesis and specifically to a method of producing 2-(2-thienyl)-3-alkyl pyrroles and N-vinyl derivatives thereof of general formula and , where Alk denotes any linear alkyl substitute. The method is a single-reactor three-component reaction of 2-acylthiophene, hydroxylamine chloride and excess acetylene in the presence of an alkali metal hydroxide with adding sodium bicarbonate to DMSO in an autoclave under acetylene pressure for 1-3 hours at temperature of 80-120°C in a wide range of molar concentration of reactants; molar ratio of reactants acylthiophene: hydroxylamine chloride: acetylene: MOH: DMSO varies in the range of 1:1.0-1.5:2-25:1.5-2.5:30-50.

EFFECT: method of obtaining novel compounds which can be used as monomers for producing electroconductive polymers, particularly as active components of electrodes of polymer rechargeable batteries and electrochromic devices.

2 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are presented nitrogen-containing heterocyclic compounds presented by the following formula wherein the radical values are specified in the description. These compounds or their pharmaceutically acceptable salts possess strong EP1 activity if introduced in a human or an animal; they are used as an effective component of a pharmaceutical agent, e.g. for preventing and/or treating overactive bladder.

EFFECT: compounds are used as an effective component of the pharmaceutical agent for preventing and/or treating the symptoms including frequent urination, heavy urination demand accompanied by fear of involuntary urination, and urinary incontinence.

24 cl, 145 ex, 5 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to a piperidine derivative of general formula (I)

,

where R1 denotes hydrogen or a substitute selected from the following (b)-(i): b) acrylic acid (including alkyl ester and hydroxyalkyl amide), (c) ureide, (d) alkenyl, (e) aminoalkyl which can be substituted with alkyl carbonyl or aminocarbonyl, (f) carbonyl alkyl, substituted with hydroxy, alkoxy or hydroxyalkylamino, (g) carbonyl, substituted with hydroxy, morpholino, alkoxy, hydroxyalkyl aminoalkoxy or cyclohexyloxy carbonyloxyalkoxy, (h) carbonylamino, substituted with alkyl or alkoxy, (i) aminocarbonyl which can be substituted with one or two substitutes selected from amino, hydroxy, alkoxy, alkenyl and alkyl (which can be substituted with halogen, thiol, piperidino, amino, alkoxy, alkoxycarbonyl, aminocarbonyl or one or two hydroxy); R2 denotes hydrogen or a substitute selected from the following (j)-(r): (j) cyano, (k) acrylic acid, (l) alkyl, substituted with hydroxy or piperidino, (m) carbonyl alkyl, substituted with hydroxy, alkoxy (which can be substituted with cyclohexyloxy carbonyloxy) or hydroxyalkylamino, (n) carbonyl, substituted with hydroxy or alkoxy, (o) carbonyl alkoxy, substituted with alkoxy, (p) carbonyl alkyl sulphanyl, substituted with hydroxy or alkoxy, (q) alkoxy, (r) halogen; and R3 denotes hydrogen or a substitute selected from the following (s)-(w): (s) alkyl which can be substituted with carboxy, cyano, pyrrolidyl, piperidino, alkoxy, alkyl sulphanyl or one or two hydroxy, (t) carbonyl, substituted with alkyl or alkoxy, (u) carbonyl alkoxyalkyl, substituted with hydroxy or alkoxy, (v) carbonyl alkyl, substituted with alkyl, alkoxy or alkylphenyl, (w) aminoalkyl, substituted with aminocarbonyl or alkane sulphonyl, where one of said R1 and R2 denotes a substitute other than hydrogen, A is unsubstituted or is an oxo, B denotes carbon or oxygen, one of X and Y denotes carbon and the other denotes sulphur, the dotted line denotes a single bond or a double bond, under the condition that when R2 denotes halogen or alkoxy, A is unsubstituted, R1 denotes a substitute other than hydrogen and B denotes oxygen. The invention also relates to an antihistamine which contains a compound of formula I and use of the described compound for treatment and production of a medicinal agent.

EFFECT: novel compounds having antagonistic action on histamine receptors are obtained and described and can be suitable as active ingredients of a pharmaceutical composition, especially an antihistamine composition.

17 cl, 40 ex, 21 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the use of compounds of formula (wherein R1, R2, X, Y and n have the values specified in the patent claim) or their pharmaceutically acceptable salts for treating the diseases related to the biological function of the trace amine associated receptors, namely depression, anxiety disorders, bipolar disorders, attention deficit/hyperactivity disorder, stress-induced disorders, schizophrenia, neurological disorders, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, addictions, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, energy consumption and assimilation disorders, thermal homeostasis disorders and disturbances, sleeping and circadian rhythm disorders, and cardiovascular diseases. Besides, the invention refers to compounds of formulas I-A, I-B, I-C, I-D, l-E, l-F, I-G, I-H (structural formulas of which are presented in the patent claim) and to a pharmaceutical composition based on the compounds of formula (I) for treating the diseases related to the biological function of the trace amine associated receptors.

EFFECT: use of the compounds of formula 1 in preparing the drugs for treating the diseases related to the biological function of the trace amine associated receptors.

45 cl, 9 dwg, 1 tbl, 379 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of 2-heteroaryl-substituted benzothiophene and benzofuran, precursors thereof and therapeutic use of said compounds, having structural formula (1a) where R1, R2, X9 and Q assume values given in the description, and pharmaceutically acceptable salts thereof, which are suitable for imaging amyloid deposits in living patients. The invention also relates to pharmaceutical compositions based on compounds of formula 1a, use and methods of producing said compounds. More specifically, the present invention relates to a method of imaging brain amyloid deposits in vivo for intravital diagnosis of Alzheimer's disease, and measuring clinical efficiency of therapeutic agents against Alzheimer's disease.

EFFECT: high efficiency of using said compounds.

15 cl, 1 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to a novel compound - 6-methyl-1-(thietanyl-3)uracil of formula 1 , which stimulates the protective activity of phagocytes.

EFFECT: obtaining compounds which stimulate the protective activity of phagocytes.

2 cl, 1 dwg, 1 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a method for preparing stabiliser-coated nanocrystalline cerium dioxide characterised by antioxidant activity. The method involves preparing an aqueous solution of cerium salt and a stabiliser representing maltodextrin with a molar ratio of cerium to the stabiliser 1 to 1-4. Then, the prepared aqueous solution is added with drops of hydrous ammonia with stirring, and pH of the prepared solution is gradually increased to 7-8, maintained for 1-4 hours, the prepared colloidal solution of hydrous cerium nanoparticles is added with hydrous ammonia, and pH is increased to 11-12 and maintained for 1-10 hours to form a colloidal solution of cerium dioxide. Thereafter, an alcohol or ketone excess is removed and brought to the boiling point, while the formed precipitate of the non-aggregated nanoparticles of stabiliser-coated cerium dioxide, separated by decantation or filtration, washed 1-4 times in alcohol or ketone, and dried at temperature 50-80°C to constant weight. The prepared powder of the non-aggregated nanoparticles of stabiliser-coated cerium dioxide is re-dispersed in a polar solvent to form aggregation resistant sol.

EFFECT: invention provides preparing stabilised nanocrystalline cerium dioxide with a hydrodynamic diameter of 6-10 nm.

3 cl, 7 dwg, 4 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine, namely to radiation biology, and may be used to treat a cadmium radiation injury and to produce a preparation for the cadmium radiation injury. Treating the cadmium radiation injury is ensured by the single subcutaneous administration of a composition consisting of anti-radiation therapeutic globulin and a suspension-forming fraction of bentonite, in a dose of 20-25 mg/kg of body weight that is followed by three more administrations 24, 48, 96 hours later if observing chronic heavy metal administration. The preparation is produced by dissolving the suspension-forming fraction of bentonite in anti-radiation therapeutic globulin in ratio 0.3:99.7 respectively while constantly stirred, and a solid concentration is reduced to 10%; the preparation is sterilised by filtration and then bottled 250-300 cm3 each to be closed tightly and kept at temperature 4-6°C.

EFFECT: method enables a consistent process of the preparation with enhanced therapeutic and decorporating effect ensured by the targeted delivery as a single agent with simplifying the use conditions.

3 cl, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is the use of L-carnosine for making a nanopreparation having antihypoxic and antioxidant activity combined with a combination of substances selected from the group of phospholipids, non-polar lipids in the following ratio, wt %: L-carnosine - 1.1-1.2, non-polar lipids such as triglycerides, cholesterol, free fatty acids, DL-α-Tocopherol - 1.2-2.5, phospholipids such as phosphatidylcholine, phosphatidylethanolamine, lysophosphatidylcholine, lysophosphatidylethanolamine, sphingomyelin - 95.3-96.3 for preparing a drug having antihypoxic and antioxidant activity. The drug can be presented in the form of liposomes containing L-carnosine.

EFFECT: invention provides higher stability of L-carnosine and its lifetime up to three days with underlying higher effectiveness in small doses, as well as to improve the cerebral ischemia tolerance, the recovery after acute hypoxia and to increase the antioxidant status of the brain tissue.

3 cl, 4 dwg

Antioxidant // 2481116

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to an antioxidant containing a cyclolanostan derivative selected from 9,19-cyclolanostan-3-ol and 24-methylene-9,19-cyclolanostan-3-ol, and a lophenol derivative selected from 4-methylcholest-7-en-3-ol, 4-methylergost-7-en-3-ol and 4-methylstigmast-7-en-3-ol, in the concentration of min. 0.0001 wt %, as an active ingredient. The invention also concerns a method for preparing the specified antioxidant. The antioxidant may be used as a drug preparation, a food or a beverage, a food additive, a drug preparation for topical skin application.

EFFECT: mentioned antioxidant provides the inhibition of lipid peroxide formation.

28 cl, 2 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to a formulation of (RS)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide possessing modulatory activity with an adequate effect, to a pharmaceutical substance of (RS)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide containing: 2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide - min. 99.0% and max. 100.5% at a dry substance; individual accompanying impurities, either single or total - max. 0.2%; the residual quantities of organic solvents, either single or total - max. 3000 ppm. The invention also refers to a method for preparing a pharmaceutical substance differing by the fact that the raw material is purified, crystallised, stabilised by treating the formulation in demineralised water that is followed by isothermal crystallisation from propanol, and drying. The invention also refers to compositions for internal and external application.

EFFECT: invention provides higher efficacy, safety, stability and width of therapeutic application.

55 cl, 3 dwg, 80 tbl, 27 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is the use of 3,5-seco-4-norcholestan-5-one oxim-3-ole, or one of its acceptable acid addition salts, or one of its esters, or one of its acceptable acid ester addition salts as an antioxidant. What is shown is that the compound possesses systemic activity per os; it does not absorb visible UV-lights and interact with common sun protection products; it is presented in the form of a crystalline powder and keeps well at room temperature for at least 12 months; it is colourless, tasteless and odour-free.

EFFECT: properties make the compound to be preferred in cosmetic and food fields, and as antioxidant preserving agent used in particular in cosmetic, food and pharmaceutical products.

9 cl, 1 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to amides of 2-(2-hydroxyphenylthio)acetic acid, having antioxidant activity, which are phenol derivatives having in the ortho-position a thioacetamide fragment of general formula: , where R1=H, Me; R2=H, CH2COOMe, CH(Me)COOMe, CH(Et)COOMe, CH(i- Pr)COOMe, CH(i-Bu)COOMe, CH(Bn)COOMe, CH(4-HOBn)COOMe, CH(CH2CH2SMe)COOMe, CH2COOH, CH(Me)COOH, CH(Et)COOH, CH(i- Pr)COOH, CH(i-Bu)COOH, CH(Bn)COOH, CH(4-HOBn)COOH, CH(CH2CH2SMe)COOH, CH2CH2CH2CH2CH(MH2)COOH, CH2CH2CH2CH(NH2)COOH; R3=H; R2R3=CH2CH2N(C(O)CH2S(2-OHPh))CH2CH2; R2,R3=CH2CH2CH2CH(COOMe); R2,R3=CH2CH2CH2CH(COOH). The invention also relates to a method of producing the said compounds.

EFFECT: compounds have antioxidant activity, which enables use thereof to reduce the rate of peroxide oxidation of lipids.

2 cl, 3 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely a therapeutic preparation of male larval bees having immunomodulatory action. The therapeutic preparation of male larval bees having immunomodulatory action possessing a yellow powder prepared by grinding male larval bees to a homogenous biomass added with an aqueous-alcohol propolis extract and fine pollen; it is followed by freezing the paste and sublimation drying in a vacuum chamber in the certain environment.

EFFECT: preparation described above shows evident immunomodulatory action.

1 tbl

FIELD: chemistry.

SUBSTANCE: compound is a pyrrolidine derivative having a fragment of a sterically hindered phenol, having general formula: where R1 denotes H, Me, Et; R2 denotes Me, Et, i-Pr, i-Bu; Ar denotes Ph, 2-HalPh, 3-HalPh, 4-HalPh, (where Hal denotes F, Cl, Br, I), 2,6-diMePh, 2,3,5,6-tetraFPh, 2-MeOPh, 3-MeOPh, 4-MeOPh, (naphthalen-1-yl), (naphthalen-2-yl), 2-NO2PH, 3-NO2Ph, 4-NO2Ph. The compounds are obtained by mixing a solution of azomethine of formula: where values of R1, R2 are given above, with N-substituted malemide in air and reaction thereof is induced by catalytic amounts of N-tert-butoxycarbonyl derivatives of alpha-amino acids (glycine, alanine, phenylalanine), followed by concentration of the organic phase at low pressure, and cleaning the residue by chromatography on silica gel using CHCl3/MeOH as the eluent.

EFFECT: prolonged antioxidant activity.

2 cl, 2 tbl, 9 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to biologically active compounds. Agent represents 3,6-dioxocyclohexa-1,4-diene-1,2,4,5-tetrasulfonate sodium. The new agent elicits antioxidant properties and therefore it can be used in food industry, in pharmaceutical compositions and cosmetic products. Also, the new agent elicits antiviral activity owing to it can be used as both the independent medicinal agent and in compositions with other preparations used for treatment of viral infections.

EFFECT: expanded assortment of medicinal agents and antioxidants, realization of indicated prescription.

1 tbl, 8 dwg

Up!