2-hydroxy-1-naphthylethylenediamine 5-nitro-2-furaldehyde exhibiting antimicrobial activity against the bacteria of the genus staphylococcus
(57) Abstract:Usage: in medicine, as an antimicrobial agent to bacteria Staphlyococcus. The inventive product 2-hydroxy-1-naphthylethylene 5-nitro-2-furaldehyde. B. F. C16H11N3O4. Tpl.200 201°C (with decomp. ) LD50more than 1000 mg/kg the Minimum inhibitory concentration of 0.07 to 1.25 μg/ml Minimum bactericidal design of 0.07 to 1.25 µg/ml, which is several times the action furazolidone. Reagent 1: hydrazone 2-hydroxy-1-naphthaldehyde. Reagent 2: 5-nitrofurfural. Process conditions: in the midst of ethanol at 50°C. table 1. The invention relates to new biologically active compounds, namely 2-hydroxy-1-naphthylethylenediamine 5-nitro-2-furaldehyde exhibiting antimicrobial activity against the bacteria of the genus Stapylococcus and which may find application in medical practice as an antimicrobial drug.In medical practice for the treatment of infections caused by gram-positive and gram-negative microorganisms used furazolidone (N-(5-nitro-2-furfurylamine)-3-aminooxy - soliton-2) formula
-N= CHNO2He belongs to the class of low-toxic substances (LD501758 mg/to the BR> However, in cases when you want more high activity and low toxicity of antimicrobial drug, it can not be used.The present invention proposes a new substance: 2-hydroxy-1-naphthylethylenediamine 5-nitro-2-furaldehyde exhibiting antimicrobial activity against bacteria of the genus Staphylococcus.The technical result of the invention is to find new substances with high antimicrobial activity against bacteria of the genus Staphylococcus and is achieved through the synthesis of the compounds of formula
This antimicrobial activity against bacteria of the genus Staphylococcus synthetic substances increases in 1,3-93 times in comparison with the practice furazolidone.Comparative analysis of the prototype shows that the claimed compound is characterized by the fact that it is a fragment of the 3-aminoquinoline-2 replaced by 2-hydroxy-1-naphthylethylenediamine.The compound obtained by condensation reaction of hydrazone 2-hydroxy-1-naphthaldehyde with 5-nitrofurfural taken in the ratio of 1:1 for 10-15 minutes according to the following reaction
< / BR>The method of obtaining the claimed matter is simple in execution, the original prophetic is dimetilformamide and dimethyl sulfoxide, little soluble in aliphatic alcohols, acetone, water, practically insoluble in ether.An example of obtaining 2-hydroxy-1-naphthylethylenediamine 5-nitro-2-furaldehyde (number of state registration 10065890 from 21.11.90).To a hot ( 50about(C) ethanol solution of 1.86 g (10 mmol) of hydrazone 2-hydroxy-1-naphthaldehyde in 70 ml of ethanol is poured a solution of 1.41 g (10 mmol) 5-nitrofurfural in 30 ml2H2HE. Almost immediately formed a yellow-orange precipitate. The reaction mixture is cooled to room temperature, the resulting material is filtered off, washed it with ethanol, ether and dried in air. The output of 2.72 g, which is 88% of theoretically calculated; TPL200-201aboutC (with decomp.).Found, With 62,01, 59,94; N 3,40, 3,51; N 13,50, 13,69.WITH16H11N3ABOUT4< / BR>Calculated With 62,14; N. Of 3.56; N 13,59.the data of IR spectroscopy, cm-1: (HE) 3450; (CH) furan 3160; (CH) 2920 cm-1; (C=N) 1630; (C=C), 1590;as(NO2) 1510, 1340; (C-O) 1320; (HE) 1240; (C-O-C) furan 1240, 1220; (C-N) 1185, 1110; and (C-N) 970, 925.Study of antimicrobial activity of compounds was carried out using twofold serial dilutions  in the liquid nutrient medium (meat-peptone broth, pH 7.0). Vesiculosa.The tests were carried out with cultures of Staphylococcus aureus (strains Wood-46, Cowan-1, Smith, 209 (H) and Staphylococcus epidermidis (42-a). For seeding used the 18-hour agar culture of these microorganisms. Sowing dose 250-500 thousand microbial cells in 1 ml of medium (optical standard turbidity). The tubes were shaken and placed in a thermostat at 243 h at 37aboutC, control served as a nutrient medium with a culture without the test chemical compound. Bacteriostatic activity was determined by the lack of growth in a nutrient medium, and bactericidal by re-seeding from tubes with no visible growth and incubation.Toxicity tests conducted in acute experiments on white mice by introducing into the stomach of suspended matter in boiled water.The results are presented in the table in comparison with antimicrobial activity used in medical practice furazolidone, a structural analogue of the claimed substance and having the highest activity among antimicrobials nitrofuranovye type.As can be seen from the table, the claimed compound exhibits high as bacteriostatic and bactericidal activity to all ispytannaya about what bacteriostatic activity it 1.3 93 times that of structural analogues. Toxicity also declare the connection as well as furazolidone can be classified as low-toxic substances.Detected properties of the synthesized compounds are of interest from the point of view of the backup extension antimicrobial agents. 2-Hydroxy-1-naphthylethylenediamine 5-nitro-2-furaldehyde formula
showing antimicrobial activity against the bacteria of the genus Staphylococcus
FIELD: oncological diseases.
SUBSTANCE: invention is designed for use in complex treatment of urinary bladder cancer in case of propagation of tumor to sub-epithelium connective tissue. Method comprises transurethral resection and introduction of immune preparations and furacillin solution. Once transurethral resection completed, three-way Foli catheter is transurethrally introduced to patient, through which mixture of standard furacillin solution with 10·106 ME interferon α-2β is injected from the first postoperative day and over following 3-5 postoperative days bringing summary dose of interferon to 50·106 ME.
EFFECT: prevented traumatism of urinary bladder due to single introduction of catheter and assured continuous action of drugs without development of immune complications.
FIELD: veterinary science.
SUBSTANCE: the suggested preparation contains the following ratio of components, weight%: dioxidine 0.48-0.52, furacrylin 0.021-0.027, dimethylsulfoxide 38-50, distilled water - the rest.
EFFECT: higher therapeutic efficiency.
3 ex, 3 tbl
FIELD: veterinary medicine.
SUBSTANCE: the present innovation deals with ways and preparations for treating and preventing acute and chronic endometritis, vaginitis, balanoposthitis. One should introduce froth-forming suppositories into cavity of affected organ, moreover, suppositories contain in their composition different medicinal substances, foaming agents, a filler, foam stabilizers and other crystalline substances reduced up to amorphous state. Moreover, components of suppositories are in the following ratio, g (weight%): potassium iodide 1.5 (6.8), furacillin 0.7 (3.2), Trikhopol (Metronidazole) 2.0 (9.0), lidocaine hydrochloride 0.8 (3.6), calcium carbonate (precipitated chalk) 2.6 (11.8), sodium bicarbonate 9.0 (41.0), calcium stearate 0.2 (0.9), common salt 1.0 (4.6), citric acid 3.0 (13.6), 20%-alcoholic solution of MGD-2 emulsifier 1.2 (5.5). The method provides prolonged complex bactericidal and antiprotozoan, antiphlogistic, local anesthetizing impact upon animal and activation of body protective system.
EFFECT: higher efficiency of prophylaxis and therapy.
FIELD: medicine, surgery.
SUBSTANCE: after sanitation one should once inject intravenously 0.04%-sodium hypochlorite solution at 10 ml/kg body weight and then - repeatedly in about 10-12 h at the same dosage; then in about 10-12 h twice and in 36 h it is necessary to perform intravenous laser blood irradiation with a He-Ne laser at the dosage of 2 mW at exposure of 5 min. The innovation enables to normalize the quantity of erythrocytes, thrombocytes and leukocytes, provides complete restoration of phagocytic and digestive capacity of neutrophilic granulocytes that, in its turn, enables to interrupt syndrome of endogenic intoxication in earlier terms.
EFFECT: higher efficiency of therapy.
1 cl, 2 ex
FIELD: veterinary science.
SUBSTANCE: invention involves the combined use of antibacterial preparations and immunomodulator. Method involves complex of single and double RNA sodium salts from killer yeast Saccharomyces cerevisiae as an immunomodulator and synthetic polymer-carrier taken in the dose 0.3-0.4 mg/kg. Immunomodulator is administrated in animals in a single dose before onset of critical period, i. e. in 15-20 days of piglets growing. Method provides stimulation of factors of cellular and humoral immunity of animals without adverse reactions and complication due to selection of optimal dose of immunomodulator and its prolonged effect.
EFFECT: improved method for treatment and prophylaxis.
3 cl, 4 tbl, 3 ex
FIELD: veterinary science.
SUBSTANCE: the suggested preparation contains enrofloxacin, dimethyl sulfoxide, furacriline and distilled water at the following ratio of components, weight%: enrofloxacin 0.3-0.5, furacriline 0.021-0.027, dimethyl sulfoxide 38-50%, distilled water - the rest. The preparation should be introduced due to intrauterine injections, in sows - with the help of special equipment for artificial insemination. Against other analogs the preparation is of wider range of anti-microbial action and high anti-microbial activity.
EFFECT: higher efficiency of therapy and prophylaxis.
6 ex, 6 tbl
FIELD: medicine, surgery.
SUBSTANCE: invention relates to a method for treatment of biliary peritonitis. Method involves abdominal cavity sanitation with furaciline, a single intravenous administration of 0.04% sodium hypochlorite solution in a patient as measured 1/10 of volume of circulating blood in patient body, and additional intramuscular administration of 10% alpha-tocopherol solution in 5-6 h as measured 100 mg per 24 h. In the following 24 h sodium hypochlorite and alpha-tocopherol solutions in above given doses are administrated in a single dose with simultaneous administration of cefatoxime in the dose 1 g, 4 times per 24 h and dalargin in the dose 2 mg per 24 h. Method provides normalization of indices of antioxidant system for early period, recovery of cell membranes and penetrability of vessels, decreasing symptoms of endocrine intoxication.
EFFECT: enhanced effectiveness of treatment method.
2 cl, 2 ex
FIELD: medicine, diagnostics.
SUBSTANCE: the present innovation deals with functional radiation diagnostics of uterine tubes, ureters, bile-excretory pathways and so on. It is necessary to carry out ultrasound research, organ's echocontrasting technique, introduction of sterile hydrogen peroxide solution in nontoxic dosage followed finally by evaluation of the results obtained. Moreover, ultrasound research should be conducted under conditions of local intracavitary anesthesia, either due to endocavitary or transabdominal access in three stages. At the first stage one should fulfill organ's echocontrasting due to introduction of a contrast sound-conducting substance into organ's cavity, fix permeability of the latter into a hollow organ under testing, adjacent organs and cavities, detect the volume and structure of a hollow organ, the availability of pathological neoplasms and evaluate functional state of an organ. At the second stage, organ's echocontrasting should be fulfilled due to introducing a sterile hydrogen peroxide solution directly into a hollow organ, according to gaseous bubbles it is necessary to evaluate anatomical structures, the availability of pathological deviations and echocontrast movement. As for the third stage, it should be carried out about 3-6 min after removing a catheter out of the cavity, due to echocontrasting the organ with residual gaseous bubbles it is possible to evaluate the state of hollow organs according to physiological movement of bubbles along the hollow organ in real period of time followed by introduction of sterile hydrogen peroxide with the help of a catheter applied under conditions of local intracavitary anesthesia, concentration of hydrogen peroxide in solution should be equal to 0.30-0.33%. The innovation enables to detect different pathology of a hollow organ, evaluate both anatomical and physiological alterations in organs.
EFFECT: higher accuracy of detection.
4 cl, 8 ex
FIELD: chemistry of organosilicon compounds, medicine, pharmacy.
SUBSTANCE: invention relates to novel compounds and their using in therapy. Invention describes compounds of the formula (I): wherein alternate values are given in the invention claim. These substances are claimed as compounds possessing antagonistic activity with respect to GnRH, and pharmaceutical composition comprising these compounds.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.
28 cl, 3 ex
SUBSTANCE: method involves cutting out mucoperiosteal flap, making curettage and antiseptic treatment. Bone defect is filled with medical composition comprising Furacilin, aminocapronic acid, dimethylsulfoxide, glycerol, Chitosan, gelatin and water. Membrane cover is applied. The membrane has Furacilin, dimethylsulfoxide, acetic acid, glycerol, Aerosyl, Chitosan and water. The wound is covered with the mucoperiosteal flap and sutured.
EFFECT: enhanced effectiveness of treatment; prolonged hemostatic, antimicrobial and wound-healing action.
SUBSTANCE: invention relates to a cooling lubricant for mechanical processing, which contains water and triethanolamine, where in order to improve the quality of the processed surface, bacterial resistance and reduce power consumption when polishing, the cooling lubricant additionally contains oleic acid, transformer oil and furacilin, with the following ratio of components, wt %: triethanolamine - 0.15-7.5; oleic acid - 0.1-5.0; transformer oil - 3.0-10.0; furacilin - 0.04-0.07; water - the balance.
EFFECT: producing bacteria-resistant cooling lubricant which reduces power consumption when polishing and is suitable for other types of mechanical processing.
1 ex, 1 tbl