Sulfate tetra-[1--oxyethyl)-2-methyl-5-nitroimidazol] zinc (ii) hydrate exhibiting bacteriostatic activity
(57) Abstract:Usage: in medicine as a means of having bacteriostatic activity. The inventive sulfate Tetra-[1 - b-oxyethyl/-2-methyl-5-nitroimidazol] zinc (II) hydrate. BF C24H16N12O21SZn, output 0,1092 g (72%). Tpl148 - 150oC. the Reagent is 1: 1 - b-oxyethyl/-2-methyl-5-nitroimidazol. Reagent 2: ZnSO7HO. Reaction conditions: in the midst of methyl alcohol. table 4. The invention relates to new derivatives of metronidazole [1-(-oxyethyl)-2-methyl-5-nitroimidazol] with bacteriostatic action and finds application in medicine.Known use as antimicrobial agent metronidazole [1,3] found that the complexes of trace elements with lekarstvennymi substances often exhibit higher activity compared to the original substances 
The disadvantages of metronidazole are: low solubility in water, volatile effectiveness against anaerobic and aerobic microflora, a number of toxic reactions  Data on antimicrobial activity of complexes of copper (II) and platinum (II) with metronidazole are missing.It is known, is therefore metronidazol taken as equivalent when determining the biological activity of the target product.The structure of the target product was proposed on the basis of research and calculations by the method of Hackelia formal charge around molecules metronidazole presented in the paper  the Positive charge 0,0374 around N-1 and the negative (-1,0012) around the N-3 suggests that the coordination of IU-1 is carried out on the nitrogen atom in position 3. Similar structure confirmed by x-ray diffraction analysis, was installed at the complex metronidazole with platinum (II).The purpose of the invention increase bacteriostatic activity and expansion steps.This goal is achieved the target product sulfate Tetra-[1-( -oxyethyl)-2-methyl-5-nitroimidazol] zinc (II) hydrate. Gross formula: C24H46N12O21SZn, molecular weight 936,08. The resulting complex is a cheesy white precipitate.The formula of the target product:
The method of obtaining the target product based on the reaction of 1-( -oxyethyl)-2-methyl-5-intorimidazole with zinc sulfate in the environment of methanol.P R I m e R 1. 0,120 g [0,0007 M] 1-(-oxyethyl)-2-methyl-5-intorimidazole dissolved in an organic solvent in the flask with a glass stopper. To the resulting solution was added 0.1 Buechner, washed, air-dried at room temperature and stored in a desiccator over CaCl2or MgSO4. The complex of 1-( -oxyethyl)-2-methyl-5-intorimidazole with zinc sulfate.Yield 72% 0,1092 g, TPL. 148-150aboutC.The data of elemental analysis, AAS and thermogravimetry are shown in table. 1.The structure of the obtained compounds was confirmed by IR and UV spectroscopy.When comparing the IR spectra of 1-( -oxyethyl)-2-methyl-5-intorimidazole and the target product, the appearance of bands, indicating the presence of water of crystallization (3450 and 1640 cm-1), as well as bands, characteristic for the ion SO42-1120, 1090, 1070, 1050 cm-1asymmetric stretching motion; 610 cm-1asymmetric deformation oscillation and is forbidden by the symmetry of the valence fluctuation 978 cm-1that indicates the distortion of the symmetry of SO42-in the coordination complex. IT is a group of the ligand participate in the complexation does not accept, as the absorption band at 3200 cm-1saved. The change in low-frequency region of the spectrum the appearance of the bands at 310 cm-1can be attributed to the formation of ties Me-nWhen comparing the camping decrease in the intensity of the bands of the electronic transitions. The presence of zinc in a complex also confirmed by qualitative x-ray fluorescence analysis.P R I m m e R 2. The bacteriostatic activity of the claimed compounds was studied against strains of Staphylococcus aureus was ATSS 25920, Escherichia coli was ATSS 1247 "Crimea", the Bacillus subtilis ADS 6633 when compared to metronidazole in vitro by the method of diffusion in ohar. The tests were performed at a dose of 0.1 LD50obtained data are presented in table. 2.P R I m e R 3. The activity of the complex with metronidazole zinc sulfate was studied on the model of salmonellosis in mice weighing 18-20 g were infected intraperitoneally suspension of the daily culture of Salmonella typhimurium N 7 number of 8.75 103a MIC.tel/ml, caused the death of 50% of mice within 7 days. One day after infection for 7 days daily, the mice were injected intramuscularly with 0.1 ml of the study drug. The concentration of drugs 100 mg/kg Control group animals were injected with sterile saline in an amount of 0.1 ml (within 7 days). It is established that the survival rate of mice in the control group was 40% with the introduction of metronidazole 50% and the introduction of the target product on day 7 after infection, 100%
P R I m e R 4. The bacteriostatic activity of the new compounds were studied in vitro on CLASS="ptx2">P R I m e R 5. The study of the toxicity of complex metronidazole with zinc sulfate conducted on nonlinear white mice with intraperitoneal route of administration.The analyte was injected once in 2-4% of freshly heated water solutions. Using the method of probit analysis according to Litchfield and Wilcoxon signed was determined the exact values of LD50and other parameters of toxicity (LD50, LD16, LD84).It is established that metronidazole and its complex compound with zinc sulfate is characterized by relatively low toxicity and in accordance with the classification of the toxicity belong to the class of low-toxic substances (see table. 4).P R I m e R 6. The effect on the system of the coupled transport of ions in the membranes of human erythrocytes was determined by red blood cell model to study the effect of pharmacological agents on the coupled transfer of anions and cations on the parameters changing the activity of potassium and pH isotonic medium with low ionic strength.It is established that the complex metronidazole with zinc sulfate caused an optimal pH in suspensions of red blood cells only at concentrations of 10-3M Received republics with zinc sulfate and allow you to recognize the absence of negative side effect of the complex with metronidazole zinc sulfate by the action of the system of the coupled transport of ions in the membranes of human erythrocytes.P R I m e R 7. Study of the influence of compensatory-adaptive reactions in the cells of the liver, kidneys, spleen were carried out on outbred mice-males weighing 18, Two groups of animals once daily was administered intragastrically metronidazole and its complex with zinc sulfate for 7 days at a dose of 6 mg/kg of the Third group of control animals. In all groups of animals were killed by decapitation under ether anesthesia on the first, third and fifth day. As objects for study at the light-optical level climbed organs: liver, kidney, spleen.It is established that the complex metronidazole with zinc sulfate in comparison with metronidazole contributes to the development of compensatory-adaptive reactions in the liver, kidney, spleen.P R I m e R 8. To study the mechanism of reducing the toxicity of metronidazole at its complexation with zinc sulfate used model of the process of fat absorption in the small intestine by electron microscopy.According to the results of electron microscopic studies found that the introduction of complex metronidazole with zinc sulfate does not cause damaging effects on the processes of absorption of fatty acids in thin kishechnika.posle does not cause disturbances in the structural and functional properties of enterocytes.Thus, the claimed compound has a high bacteriostatic activity, low toxicity and a broader spectrum of activity than metronidazole. Sulfate Tetra-[1-( b-oxyethyl)-2-methyl-5-nitroimidazol] zinc (II) hydrate formula
< / BR>exhibiting bacteriostatic activity.
FIELD: organic chemistry, medicine, dermatology.
SUBSTANCE: invention relates to zinc and aliphatic halogen-carboxylic acid salts that can be used in treatment of benign neoplasms of skin and visible mucosa tissues. Invention proposes the following formula of zinc and aliphatic halogen-carboxylic acid salts: (1): wherein R means -CHal3, -CHHal2, -CH2Hal and (2): wherein R' means Alk, hydrogen atom (H); R'' means Hal; R' means Alk; R'' means H, Alk wherein in these formulae halogen atom can be represented by fluorine atom (F), chlorine atom (Cl), bromine atom (Br) or iodine atom (J). Invention provides the development of original preparation used in treatment of benign neoplasms of skin and visible mucosa tissues with low toxicity, rapid effect, expressed therapeutic effect and eliciting good tolerance, absence of complications in treatment, healing without formation of scar tissue. The development of the preparation provides expanding assortment of agents used in treatment of such diseases.
EFFECT: enhanced and valuable properties of agents.
FIELD: veterinary science.
SUBSTANCE: the present innovation deals with applying a multi-purpose complex preparation that contains the following components in 1 l of distilled water: sodium selenite 1.0; vitamin E/in the form of combinal E/7500 mg; succinic acid 10.0; zinc sulfate 10.0 and pharmazine 50000 U. The preparation should be introduced as intramuscular injections 45, 30, 15 d before delivery and during the day of delivery: in cows per 10-15 ml, for pigs and sheep per 5 ml, for youngsters after the birth: in calves - 5 ml, in piglets and lambs per 1-2 ml, in hens per 0.5 ml once/2 wk. The innovation is very efficient in increasing the quality and quantity of production, improving the growth and development in fetus and offspring, preventing some surgical and obstetric-gynecological pathologies.
EFFECT: higher efficiency of correction.
FIELD: veterinary science.
SUBSTANCE: invention relates to a composition used in prophylaxis and treatment of anemia in agricultural animals and poultry that comprises a mixture of chelates of iron, copper, zinc, cobalt, sodium, calcium with ethylenediamine-N,N'-disuccinic acid in the following ratio of components, wt.-%: copper chelates with ethylenediamine-N,N'-disuccinic acid, 0.45-0.60; zinc chelates with ethylenediamine-N,N'-disuccinic acid, 1.40-1.45; cobalt chelates with ethylenediamine-N,N'-disuccinic acid, 0.075-0.08; sodium chelates with ethylenediamine-N,N'-disuccinic acid 42.0-44.0; calcium chelates with ethylenediamine-N,N'-disuccinic acid, 12.0-13.0, and iron chelates with ethylenediamine-N,N'-disuccinic acid, the balance. Agent provides enhancing the blood hemoglobin content in animals by 28% as compared with animals receiving neither anti-anemic agents and by 12% as compared with animals receiving the preparation-analog.
EFFECT: enhanced effectiveness of composition.
4 tbl, 4 ex
SUBSTANCE: the present innovation deals with obtaining compositions being of bactericidal, antiphlogistic, regenerating, antioxidant and antimicrobial properties at no allergic action. Wound-healing preparation (variant 1) contains: stearic acid 4.5-6.0; purified lanolin and its derivatives 3.0-6.0; vegetable oil 3.0-5.0; Vaseline 1.5-2.5; glycerol 4.0-8.0; castor oil 8.0-12.0; zinc stearate 1.0-2.5; 70%- alcoholic extract of phytospecies 2.5-3.5; extract of common John's wort grass 3.5-8.5; dog rose oil or sea buckthorn oil 2.6-6.0; Na-salts of fatty acids of wool fat 0.3-0.6; triethanolamine 0.7-1.1; anesthesin 2.0-3.0; 10%-butyric solution of propolis 0.3-1.0; boric acid 0.4-0.6; purified water - the rest. Wound-healing preparation (variant 2) contains: stearic acid 4.5-6.0; purified lanolin and its derivatives 3.0-6.0; vegetable oil 3.0-5.0; Vaseline 1.5-2.5; glycerol 4.0-8.0; castor oil 8.0-12.0; zinc stearate 1.0-2.5; 70%-alcoholic extract of phytospecies 2.5-3.5; extract of common John's wort 3.5-8.5; dog rose oil or sea buckthorn oil 2.6-6.0; Na-salts of fatty acids of wool fat 0.3-0.6; triethanolamine 0.7-1.1; anesthesin 2.0-3.0; levomycetin or gentamycine 2.0-3.0; 10%-butyric solution of propolis 0.3-1.0; boric acid 0.4-0.6; purified water - the rest. Additional introduction of the extract of common John's wort has increased antioxidant properties; 10%-butyric propolis - antioxidant and bactericidal properties, and levomycetin and gentamycine - has widened the range of antimicrobial action. Application of the preparation suggested in patients with burns and wounds revealed positive therapeutic effect without any cicatricial neoplasms and allergic action. No contraindications had been established.
EFFECT: higher efficiency of application.
4 cl, 8 ex
SUBSTANCE: invention relates to application of Acizol, namely bis(1-vinylimidazole) zinc diacetate as coronary active anti-ischemia and anti-arrhythmia agent. Acizol makes it possible to limit development of necrosis zone in acute myocardium ischemia, to reduce frequency of complications and fatal cases, to normalize antrioventricular and intraventricular electrical conductivity , to prevent ciliary arrythmia.
EFFECT: improved anti-ischemia and anti-arrhythmia agent.
15 tbl, 7 dwg, 6 ex
SUBSTANCE: method involves administering Acizol (bis1-vinyl imidazole zinc diacetate).
EFFECT: stable remission; improved bone tissue resorption in postoperative period; accelerated periodontium tissue recovery.
3 dwg, 3 tbl
FIELD: chemical-pharmaceutical industry, metalloorganic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to polyacrylic acid incomplete zinc salt corresponding to the formula: (-CH2-CHCOOH-)n(-CH2CHCOOZn0.5-)m wherein n = 12000-35000; m = 1650-6650 wherein the content of zinc is (6-8 wt.-%) 0.0009-0.0012 g-at, the content of carboxyl groups is 0.0117-0.0122 g-equv/1 g of polymer, and molecular mass is in the limits 1000000-3000000 Da. Also, invention proposes a method for preparing this salt that involves addition of zinc acetate aqueous solution to polyacrylic acid solution, stirring the reaction mixture for 120-300 min and drying the prepared solution under vacuum at temperature 50°C, not above. Agent is prepared as a solution in the ratio 1-10 g of polyacrylic acid incomplete zinc salt in 100 ml of water. Agent shows antiseptic, hemostatic and wound-healing effect in its external using.
EFFECT: improved preparing method, valuable medicinal properties of agent.
3 cl, 1 tbl, 4 ex
SUBSTANCE: it is necessary to carry out complex medicinal therapy including specific antiviral preparations, group B-vitamins, immunocorrectors, injection of antiherpetic vaccine, and, also local therapy with derinate. Additionally, since the 1st d of exacerbation it is important to inject flosteron once i/m at 1.0 ml, cefotaxym i/m twice daily per 1.0 mg for 10 d. Immunomodulator halavit on the 1st d should be prescribed i/m at the dosage of 200 mg, and then for the next 15 d - twice daily per 100 mg i/m. Diazepam for 1 mo should be injected per 5.0 mg 4 times daily, and then per 2.5 mg 4 times daily for 1 mo, as well. One should daily inject atarax per 100 mg nocturnally for 1 mo and ketorol internally per 10 mg thrice daily for 10 d. Moreover, it is necessary to apply the composition out of 50.0 g zinc oxide, 5.0 ml ACD fraction and 25.0 g "Aciclovir" cream 4 times daily for 10 d. The innovation enables to considerably increase the efficiency of therapy due to improving the main immunological values, weakening local autoimmune reactions and, also, preventing the development of psychic disorders in such patients due to affecting viral neurotropic properties.
EFFECT: higher efficiency of therapy.
3 dwg, 1 ex
FIELD: medicine; dental surgery.
SUBSTANCE: for this purpose first of all root canals are filled with paste based on eugenol, zinc oxide, dry iodoform and lincomycin hydrochloride taken in ratio 3:3:1:1. Then cortical plate trepanation and cyst membrane extraction are followed with ultrasonic treatment of bone cavity through 0.05% miramistine within 5 minutes using ultrasonic device US-102 at exposure intensity 0.05-0.4 Wt/cm in pulse mode. Treated bone cavity is introduced with filling-bandage "Collost" and with mixed osteoplastic gel "Collost" and lincomycin hydrochloride taken in ratio 2:1, and is covered with membrane "Collost". Wound is isolated from mouth cavity with film "Dyplene-denta" with lincomycin.
EFFECT: enables to accelerated wound healing process due to complete osteointegration and angioosteogenesis of implanted material.
FIELD: medicine; pharmacology.
SUBSTANCE: composition for prevention and treatment of asthma and upper airways diseases is characterised by that it includes incense tree Boswellia serrata dry extract solution with Boswellia acids content in terms of β- Boswellia acid not less than 80%, in wheat germs oil mixed with pharmaceutically acceptable selenium source and encapsulated containing glycerine, gelatin, pharmaceutically acceptable zinc source and chicory dry extract. Composition production implies that pharmaceutically acceptable zinc source, chicory dry extract gelatin, glycerine are sequentially dissolved renovated water. Agitated mixture is used to make capsule thereafter filled with capsulation solution produced by stirring of wheat germs oil and pharmaceutically acceptable selenium source followed by gradual addition of incense tree Boswellia serrata dry extract, with Boswellia acids content in terms of β- Boswellia acid not less than 80% till it is completely dissolved. Produced capsules are kept at temperature 5-10°C and dried out.
EFFECT: produced composition has improved efficiency.
4 cl, 4 ex
FIELD: chemistry of organometallic compounds, chemical technology.
SUBSTANCE: invention relates to the improved method for preparing the chelate compound bis-(1-vinylimidazole)zinc diacetate (I) representing the medicinal preparation of acizol that is the effective antidote and antioxidant. Method for preparing the compound (I) is carried out in the absence of organic solvents at temperature 20-35°C in the mole ratio 1-vinylimidazole : zinc diacetate in the range from 10:1 to 3:1. Method provides exclusion fire hazard and explosion hazard solvent from the technological process and enhancement of the yield of highly pure acizol satisfied for Pharmacopoeia requirements.
EFFECT: improved method for preparing.
2 cl, 4 ex
FIELD: luminescent materials.
SUBSTANCE: invention provides novel electroluminescent material comprised of injecting layer, metal chelate complex-based active luminescent layer, hole-transition layer and hole-injecting layer. Luminescent substance is selected from oxyquinolate metallocomplexes of zinc 8-hydroxy-2-methoxyquinolate and zinc 8-hydroxy-2-methylquinolate. Electroluminescent material shows emission in green spectrum region.
EFFECT: increased heat resistance and widened choice of stable green-emitting materials.
2 cl, 3 ex
FIELD: organic chemistry, medicine, oncology.
SUBSTANCE: invention relates to photosensitizing agents used in photodynamic therapy of neoplasm and some other diseases. Invention describes tetraazachlorines of the general formula: wherein R1R2 mean -C6H4; R3 = R4 = R5 mean -CH3; M means HH (H2TBTAC); R1R2 means 1,2-C10H6; R3 = R4 = R5 mean -CH3; M means Zn(Zn-1,2-TNTAC); R1 = R2 mean -C6H5; R3 = R4 = R5 mean -CH3; M means HH (H2TACPh6); R1 = R3 mean hydrogen atom (H); R2 =R4 mean -C6H5; R5R5 mean -CH2N(CH3)CH2; M means HH (H2PyrTACPh4); R1R2 mean 4-C(CH3)3C6H3; R3 = R4 mean hydrogen atom (H); R5R5 mean -CH2N(CH3)CH2; M means HH (H2TBtTACPyrN-Me) used as photosensitizing agents in the near IR-region of spectrum for carrying out the photodynamic therapy. These photosensitizing agents possess the intensive absorption in spectral region 710-750 nm and can be used in treatment of deep tumor tissues by the photodynamic therapy method.
EFFECT: valuable medicinal properties of compounds.
1 cl, 4 ex
FIELD: production of high temperature superconductors.
SUBSTANCE: invention relates to electrochemical synthesis of metal β-diketonates, in particular acetylacetonates. Synthesis of Cu(II) and Zn(II) acetylacetonates in carried out by electrolysis of acetylacetone solution and base electrolyte in acetonitryl in ratio of (1:10):0.5:100, with electrodes made of metal presenting in produced acetylacetonate, at current density not more mA/cm2 by using pulse current. Pulse time is controlled by pulse forming unit connected in parallel to elecrtolyzer. As base electrolyte preferably lithium perchlorate or lithium chloride is used.
EFFECT: controlled process for production of metal acetylacetonates.
5 cl, 2 ex, 1 dwg
FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention relates to the improved method for synthesis of zinc phthalocyanine of high purity degree that can be used as a photosensitizing agent for photodynamic therapy. Method is carried out by interaction of phthalonitrile with zinc salt at heating in the presence of a tertiary amine - N,N-dialkylaniline, N,N-dialkylethanolamine or trialkylamine in an aprotonic dipolar solvent medium, for example, dimethylformamide. Method provides preparing the end product with 97-99% content of the basic substance. Method shows the technological effectiveness as it suggests using inexpensive reagents, small amount of solvent and it doesn't require the complex purifying procedures.
EFFECT: improved method of synthesis.
2 cl, 4 ex
FIELD: chemistry, chemical technology.
SUBSTANCE: invention relates to quaternized phthalocyanines and their using for treatment of water against bacterial pollution. Invention describes novel quaternized phthalocyanines representing poly-(trialkylammoniomethyl)-substituted zinc and aluminum phthalocyanines that are sensitizing agents in formation of singlet oxygen by effect of visible light. Also, invention relates to a method for photodisinfection of water by using these quaternized phthalocyanines or their mixtures with dyes of acridine, rhodamine or phenothiazine series and radiation in visible range in the presence of oxygen that provides the effective treatment of water against bacterial pollution.
EFFECT: valuable properties of compounds, improved method of water treatment.
3 cl, 5 tbl, 16 ex
FIELD: medicine, in particular photosensitizing agents for photodynamic therapy.
SUBSTANCE: invention relates to quaternary phthalocyanines of general formula MPc(CH2X)nCln, wherein Pc is phthalocyanine rest C32H16N8; M is Zn, AlY; n = 6-8; X is Y is Cl, OH, OSO3H, useful as photosensitizing agents in photodynamic therapy having high photoinduced activity in vivo and in vitro.
EFFECT: new class of effective photosensitizing agents useful in treatment of various tumors by photodynamic therapy.
1 dwg, 8 ex
FIELD: medicine, in particular photosensitizing agents for antimicrobial photodynamic therapy.
SUBSTANCE: invention relates to new photosensitizing agents for antimicrobial photodynamic therapy namely cationic phthalocyanines of general formula MPc(CH2X)nCln, wherein Pc is phthalocyanine rest C32H16N8; M is Zn, AlY; n = 6-8; X is Y is Cl, OH, OSO3H. Claimed agents is characterized by wide range of antimicrobial activity. Single complex action of nontoxic in darkness micromolar (up to 2.0 muM) concentration thereof and low dose of red irradiation make it possible to produce high inactivation levels (up to 97-99 %) both gram-negative bacteria and yeast fungi of genus Candida.
EFFECT: improved agents for treatment of various severe complications of inflammation diseases.
3 dwg, 13 ex, 2 tbl