Medication, possessing diuretic action

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutics, namely to application of P-methyl-phenyl-O-D-glucopyranoside as medication, which has a diuretic action, which has high diuretic and low saluretic activity.

EFFECT: obtaining medication, which has a diuretic action, which has high diuretic and low saluretic activity.

1 tbl, 1 ex

 

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, in rats. (Bryukhanov V.M., Zverev AF Side effects of modern diuretics: Metabolic and toxic-allergic aspects of Novosibirsk.: CARES, 2003. - 224 S.).

The closest to the achieved result is a tool that has diuretic de is predetermined, 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 by the use of P-methyl-phenyl-O-D-glucopyranoside as a means possessing diuretic properties.

Description of the invention

The inventive tool is a P-methyl-phenyl-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, an equimolar amount of p-cresol and heated at 120-130° 1.5 hrs to full the th dissolution of 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 p-cresol 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 of 4-were-2,3,4,6-Tetra-O-acetyl-D-glucopyranoside. The precipitate is filtered off.

To a suspension containing 2 g of 4-were-2,3,4,6-Tetra-O-α-acetyl-D-glucopyranoside in 5 ml of absolute methanol, add 0.5 ml of 2 n solution of sodium methylate, the mixture shaken until complete dissolution of the precipitate, then leave at 5°C for 18 hours After 15-20 min is the selection of crystals of P-methyl-phenyl-O-D-glucopyranoside. The solvent is distilled off, the residue is recrystallized from methanol. Yield: 14%.

The NMR spectra of the proposed drug:

An NMR spectrum1H (DMSO), δ, ppm,: 1.63 (3H, s, CH3), 3.14-3.30 (4H, m, H-2', H-3', H-4', H-5'); 3.66 (2H, d, H-6'a, J=11.4 Hz); 4.82 (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, top is raised the signal of solvent.

An NMR spectrum13C, (DMSO), δ, ppm: 25.1 (CH3), 60.7 (CH2, C6'); 69.2 (CH, C-4'); 73.3 (CH, C-2'); 76.6 (CH, C-3'); 77.1 (CH, C-5'); 100.5 (CH, C-1'); 116.2 (2CH, C-2, C-6); 121.8 (CH, C-4); 129.1 (2CH, C-3, C-5); 158.0 (CH, C-1).

The NMR spectra of1H,13C 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 medium was considered dost is true, if the confidence value (P) was less than 0.05.

The table presents comparative characteristics of diuretic activity of P-methyl-phenyl-O-D-glucopyranoside. Diuretic activity of P-methyl-phenyl-O-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 1.5 or more times, compared with the control. Excretion of sodium and potassium ions under the influence of the compounds according to the invention is significantly decreased starting from the 3rd day of the experiment.

Thus, the claimed product has a pronounced diuretic activity and is applicable for 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.

Table 1.
A means with diuretic
The day of introduction of the analyte of interestIndicators of kidney function
Daily diuresis The excretion of sodiumExcretion of potassium
Control2,42±0,3329,71±9,66451,41±45,27
1 day3,93±0,53*33,33±10,44618,33±69,25
P<0,05P<0,05
day 2to 4.38±0,54*--
P<0,01
3 day4,34±0,55*9,49±1,59321,67±41,14*
P<0,01P<0,05P<0,05
day 4of 4.44±0,51*--
P<0,01
5 day3,84±0,719,19±2,00*315,53±49,54*
P<0,05P<0,05
6 is Yan 3,76±0,70--
day 75,17±0,68*of 7.96±0,83398,99±33,68
P<0,01P<0,05
Note. The asterisk is a difference significantly compared to control.

The use of P-methyl-phenyl-O-D-glucopyranoside of the formula

as a means possessing diuretic.



 

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