Use of 2-amino-7-bromo-4-acetylazo[5,4-b]indol to protect organism against hyperbaric and hematic hypoxia and/or liver against carbon tetrachloride poisoning

FIELD: pharmaceutical industry.

SUBSTANCE: invention proposes use of 2-amino-7-bromo-4-acetylazo[5,4-b]indol depicted by formula: against hyperbaric and hematic hypoxia and protection of liver against carbon tetrachloride poisoning. Use of this compound reduces concentration of AlAT by a factor of 2.6 and that of AcAT by a factor of 1.67.

EFFECT: increased therapeutic activity.

3 tbl

 

The invention relates to the use of 2-amino-7-bromo-4-acetylthiazole[5,4-b]indole of formula 1

to protect the body from exposure to hypobaric and himicheskoi hypoxia and liver from poisoning by carbon tetrachloride.

This property suggests the possibility of using this compound for prevention and treatment in humans acute inhalation poisoning pairs of carbon tetrachloride. Widespread use of carbon tetrachloride in industry, agriculture and military Affairs that makes urgent the search for pharmacological agents that protect the body from exposure to this toxicant. To restore liver function used Essentiale, but its activity is insufficient.

Previously installed hepatoprotective activity of the hydrobromide of 2-amino-4-acetylthiazole[5,4-b]indole (Patent 2076867 RF, MKI36 07D 478/04, AK 31/40. The hydrobromide of 2-amino-4-acetylthiazole[5,4-b]indole protecting the liver from carbon tetrachloride poisoning and how to obtain it / Velieva B.C., Melman A... Tomchin A.B., Smirnov A.V., acavity SV, Gaivoronsky V.V. (Russia). - 5042409/04; Claimed 19.05.92.), formula 2.

Analog antihypoxic action is reference antihypoxic drug antizol formula 3 (Methodological recommendations what about the experimental study of drugs, the proposed clinical study as a antihypoxic funds./Edited Ludlowkoeni. - M: BI, 1990. - 18 C.). Hypobaric hypoxia occurs when the lack of oxygen due to reduced atmospheric pressure. These phenomena are common when we are forced to find people in the highlands or in the depressurization of the aircraft.

Himicheskaya hypoxia develops when injected into the blood of toxins, blocking the work of hemoglobin, resulting in impeded the transport of oxygen in the body and death. Poisoning of this kind is not uncommon in case of emergency chemical industries, military conflicts.

The aim of the invention is the use of compounds of indole fused with thiazole, effectively protect the body from hypoxic and hypercapnic hypoxia and liver from poisoning by carbon tetrachloride.

The inventive compound is a white crystalline substance, it is difficult soluble in water, alcohol, acetone and slightly soluble in dimethylformamide and dimethylsulfoxide. The inventive compound is produced by the action of an alkaline agent to the hydrobromide of 2-amino-7-bromo-4-acetylthiazole[5,4-b]indole.

Example. 3.0 g (to 7.67 mmol) to the hydrobromide of 2-amino-7-bromo-4-acetylthiazole[5,4-b]indole suspension in 19 ml of the odes and add 30% aqueous sodium acetate solution to pH 5-6 by the universal indicator, mix and after 30 minutes, filtered. The precipitate was washed with water (5×10 ml), dried in air and 30 min at 105°C. Obtain white crystals, the weight of 2.08 g (87,5%). For analytical purposes the substance periostat of DMF (activated carbon) in a five-fold volume of ether. The next day filtered off the precipitated crystals, washed with acetone and dried. Get shiny white crystals. Sample of Beilstein negative. The melting temperature depends on the temperature entered into the device. In the case of application at 230°With the substance melts at 250-252°C (decomposition).

The substance is homogeneous according to TLC. The adsorbent - Silufol UV-254, the solvent for application - dimethylformamide, eluent is acetone:hexane = 1:1; Rf0,64.

Range of PMR in DMSO d6. 300 MHz, ppm: 2.70 (INSN3), 6.80 (2H, NH2), 7.32 (1H, H6), 7.72 (1H, H8), 8.06 (1H, H5).

Study of biological activity of the claimed compounds. Acute toxicity was determined on outbred mice-males weighing 18-22 g by well-known methods (Prozorovsky V.B. have been and others, "rapid method for determining the average effective dose and its errors, Pharmacology and toxicology, 1978, No. 4, s-502). The target compound was administered intraperitoneally once in suspension in water with the addition of tween-80. LD503890±370 mg/kg, which can be attributed to the claimed little connection to execmem substances.

Study of the protective effect of compound 1 when exposed to hypobaric hypoxic hypoxia. Experiments were performed on outbred mice weighing 18-20 g of the Inventive compound was administered intraperitoneally in the form of a thin slurry with divinam-20 dose of 67.1 mg/kg 30 minutes prior to the hypoxic episode. The optimal dose was chosen based on preliminary experiments. The effect of the drug was compared with known antihypoxic drug-antisolar in equimolar dose of 25 mg/kg to Mice in the control were treated with equivalent volumes of saline. In each group of 6 animals.

Hypoxia was simulated in the chamber "lifting" of the animals at the altitude of 10,000 m with a speed of 50 m/s and an exposure time within 90 minutes assessment of the protective effect was studied by life expectancy and survival of animals after a hypoxic episode. The activity of the claimed compounds 1 in comparison with the known analogue presented in table 1.

Table 1
Antihypoxic activity of the claimed compounds
ConnectionThe average life expectancy minIncrease survival of animals %
Control5,06±2,170
Antizol75*
Connection 116,0083*
Note. The difference is significant in comparison to the control animals *-R≤0,01.

According to table 1 it is seen that the inventive compound 1 increases survival of animals in 3.16 times compared to control (antizol in 4.15 times), but the number of surviving individuals at him more than the benchmark (83% and 75% respectively). Therefore, we can conclude that the connection exceeds 1 for this type of activity reference drug.

Gemicescuu hypoxia (Manual on experimental (preclinical) study of new pharmacological substances. Moscow (2000), 153-158) was studied on mice-males weighing 18-20, study drug in equimolar dose in relation to antipolo was injected intraperitoneally in the form of a thin slurry with tween-20 for 30 minutes before hypoxia, which was modeled by the introduction of intraperitoneally 2% solution of sodium nitrite at a dose of 200 mg/kg the Effect of the drug was compared with known antihypoxic drug-antisolar at a dose of 25 mg/kg to Mice in the control were treated with equivalent volumes of saline. Register the lifetime of animals and the number of surviving individuals. The activity of the claimed compounds 1 in comparison with the known analogue presented in table 2.

Table 2
Antihypoxic activity of the claimed compounds on the model himicheskoi hypoxia
MedicationDose, mg/kgQty animalsLifetime minLife expectancy % compared to the controlThe increase in survival rate, %
Phys. solution-729,83±to 10.09--
Antizol25,0643,07±7,21*144,4-
Connection 167,1658,44±24,21*195,550,0**
Note. The difference is significant in comparison to the control animals *-R≤0,05, **-R≤0,01

The results of the experiments are given in table 2, show life expectancy of animals are almost two times (the standard one and a half times), but the connection 1 helps to survive half of the individuals, and the standard does not give survival. The claimed connection far exceeds antizol on antihypoxic activity on the model himicheskoi hypoxia.

Hepatotropic action was studied on rats male weight 140-170, carbon Tetrachloride was injected PADCO is but daily in 50% solution in liquid paraffin for 4 days in a row in an amount of 0.4 ml/100 g mass. Simultaneously with CCl4introduced compound 1 at a dose of 67.1 mg/kg intraperitoneally. It was compared with the known hepatoprotector Essentiale and compound 2, which was investigated in equimolar dose of 67.6 mg/kg

The clinical picture of poisoning CCl4develops slowly. The main symptoms of severe intoxication is manifested only at the end of 2 days, and in 4 to 7 days lead to a lethal outcome. All the patients had severe liver damage up to fatty degeneration of the body. Evaluation of the protective effect of compounds 1 and analogues was performed by examining the activity specific for liver alanine transferase (Alt) and aspartate aminotransferase (AST) in the serum. The change in the activity of Alt and AST in the serum indicates deleterious effects CCl4on the cell membrane and organelles of the cell. The results of the experiments are shown in table 3.

105
Table 3.
The change in the activity of Alt and AST in the serum on the seventh day of the experiment
Groups of animalsB %AST, %
The intact100100
CCl4281151
CCl4+Essentiale127
CCl4+connection 110990
CCl4+connection 2151120

The data obtained indicate that the use of compound 1 in 2.6 times reduces the concentration of Alt and 1.67 times the concentration of AST. Thus, the ability to protect the liver from poisoning by carbon tetrachloride connection exceeds 1 connection 2 and table.

The use of 2-amino-7-bromo-4-acetylthiazole[5,4-b]indole of the formula

,

to protect the body from hypobaric and himicheskoi hypoxia and/or liver from poisoning by carbon tetrachloride.



 

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