Diuretic agent

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is an agent of diuretic action of a group of aquaretics, phenyl-α-O-D- glucopyranoside. The agent may be used both to treat greater and lesser circulation congestions caused by cardiac failure, and to intensify water release thereby helping to reduce oedemas. The agent has high and low saluretic activity unlike the existing diuretics and expands the range of products of synthetic origin possessing diuretic activity.

EFFECT: agent is applicable for treating the number of cardiovascular diseases accompanied by excessive hydration and developing oedema syndrome.

1 tbl

 

The invention relates to pharmacology, namely a drug with diuretic group of aquaretic and can be used to treat nephritis, pielonefritom, cystitis, hypertension, symptomatic hypertension, diseases, accompanied by the development of edema syndrome, as this substance increases the excretion of water, thereby reducing the swelling.

Currently, there is a need to develop diuretics, high diuretic activity and low toxicity. Of particular interest is the creation of medicines, which has diuretic and does not affect the allocation of kidneys ions of sodium, potassium, magnesium.

It is known tool that has a diuretic effect, namely, ethacrynic acid, which is used as a selective antagonist of sodium-potassium-glastransporter (NKCC).

The disadvantage etakrinova acid is the high toxicity and the absence of diuretic action in animals, for example rats (Bryukhanov V.M., Zverev AF Side effects of modern diuretics: Metabolic and toxic-allergic aspects - Novosibirsk: CERES, 2003. - 224 S.).

The closest to the achieved result is a tool that has diuretic dei is a journey, namely furosemide.

Lack of furosemide in the first place is salureticheskoe activity. Like all loop diuretics, furosemide inhibits the reabsorption in the renal reabsorption of sodium, potassium and chloride. In addition, furosemide causes such metabolic disorders as hypokalemia, gipohloremicski alkalosis, hyperglycemia, hyperuricemia (Zverev AF, Bryukhanov V.M. Pharmacology and clinical use extrarenal action of diuretics - M: Medical book, 2000. - 256 S.).

The technical result of the proposed drug is the expansion of the means of possessing diuretic activity of synthetic origin.

The technical result is achieved that apply Phenyl-α-D-glucopyranoside as a means possessing diuretic properties.

Description of the invention

The inventive tool is a Phenyl-α-O-D-glucopyranosid, the following formula:

This glycoside synthesized by alloying with aluminum. The structure was proved by NMR. Acyl protection was removed with sodium ethylate.

The inventive tool is obtained as follows: in a three-neck flask equipped with stirrer, reflux condenser and thermometer, is placed 0.2 g of aluminum foil, equimolar quantity of phenol and heated at 120-130° 1.5 h to complete restorani is aluminum. To the resulting phenolate are added to 3.9 g 1,2,3,4,6-Penta-O-acetyl-D-glucopyranose and heated for 2 h to 140-150° with continuous stirring. After 2 hours the reaction mass is then cooled to 60°, dissolved in chloroform (20 ml) and the chloroform solution is washed with 0.1 n sulfuric acid (10 ml ×2 times), of 0.1 n sodium hydroxide (10 ml ×2 times) and water (10 ml ×2-3 times) to remove excess phenol and aluminum. The chloroform layer is dried over sodium sulfate. Then the chloroform is distilled off. The oily residue is recrystallized from alcohol. Fall white crystals phenyl-2,3,4,6-Tetra-O-acetyl-D-glucopyranoside. The precipitate is filtered off.

To a suspension containing 2 g of phenyl-2,3,4,6-Tetra-O-α-acetyl-D-glucopyranoside in 5 ml of absolute methanol, add 0.5 ml of 2n solution of sodium methylate, the mixture shaken until complete dissolution of the precipitate, then leave at 5° for 18 hours After 15-20 min is the selection of crystals phenyl-O-D-glucopyranoside. The solvent is distilled off, the residue is recrystallized from methanol. Output: 12%.

The NMR spectra of the proposed drug:

An NMR spectrum1H (DMSO), δ, ppm: 3.13-3.33 (4H, m, H-2', H-3', H-4', H-5'); 3.66 (2H, d, H-6', J=11.4 Hz); 4.83 (1H, d, H-1', J=6.9 Hz); 6.96 (3H, m, H-2, H-4. H-6); 7.26 (2H, m, H-3, H-5). Not specified signal of the proton H-6'b, overlaps with the signal of solvent.

An NMR spectrum 13(DMSO), δ, ppm: 60.7 (CH2, C6'); 69.7 (CH, C-4'); 73.2 (CH, C-2'); 76.6(CH, C-3'); 77.1 (CH, C-5'); 100.3 (CH, C-1'); 116.2 (2CH, C-2, C-6); 121.8 (CH, C-4); 129.4 (2CH, C-3, C-5); 157.1 (CH, C-1).

The NMR spectra of1H,13With were recorded on FTIR spectrometer Bruker Avante-300 (300 MHz), Bruker (Germany) internal standard HMDS, the solvent used deuterated acetone. The melting point was determined on microsegregation table Boetius company Boetius (Germany).

The resulting tool is characterized by the following properties: white crystals. Soluble in water, alcohol, chloroform.

Pharmacological action the proposed drug tested by biological research. Activity funds were estimated at 12 laboratory rats-females weighing 200-220 grams. In the beginning of the experiment were determined baseline urine output, as well as the content of sodium and potassium in the urine of experimental animals. The concentration of ions in the urine were determined by flame photometry on the analyzer the FCA-2-01 (Russia). The analyte was injected to rats intragastrically for seven days at a dose of 54 µmol/kg Daily in experimental animals was measured volume of allocated urine. The experimental results were processed by the statistical method using the criterion of Mann-Whitney. The difference compared averages were considered significant if the show is spruce reliability (R) was less than 0.05.

The table presents comparative characteristics of diuretic activity of Phenyl-α-D-glucopyranoside. Diuretic activity of Phenyl-α-D-glucopyranoside at a dose of 54 µmol/kg

As can be seen from table 1, the introduction of the compounds according to the invention increased daily diuresis in 2 and more times compared with the control. The excretion of sodium ions under the influence of the compounds according to the invention had a tendency to increase, but all the changes compared to the control were not statistically significant. Excretion of potassium ions increased by not more than 3 times compared to the control throughout the experiment.

Thus, the claimed product has a high diuretic, low salureticheskoe activity and applicable to the treatment of stagnant phenomena in small and large circle circulation caused by congestive heart failure, nephritis, cirrhosis of the liver with symptoms of portal hypertension, hypertension, symptomatic hypertension, glaucoma and other diseases associated with development of edema syndrome.

The use of Phenyl-α-D-glucopyranoside of the formula

as a means possessing diuretic.



 

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1 tbl, 1 ex

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