6-methyl-1-(thietanyl-3)uracil stimulating protective activity of phagocytes

FIELD: chemistry.

SUBSTANCE: present invention relates to a novel compound - 6-methyl-1-(thietanyl-3)uracil of formula 1 , which stimulates the protective activity of phagocytes.

EFFECT: obtaining compounds which stimulate the protective activity of phagocytes.

2 cl, 1 dwg, 1 tbl, 2 ex

 

The present invention relates to organic chemistry and medicine, in particular to a new connection - 6-methyl-1-(titanyl-3)uracil, stimulating protective activity of phagocytes.

As a prototype, and the comparison drug taken methyluracil (beta-form 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine), used in medicine [Mashkovsky PPM Medicines. // M, LLC "New wave", 2004, Vol.2, p.160-161], is known as a means for activation of alveolar macrophages [patent RU 2063226, 1996].

The objective of the invention is to expand the Arsenal of biologically active substances, including with their phagocytic activity.

The technical result - obtaining biologically active substances that stimulate protective activity of phagocytes.

The inventive 6-methyl-1-(titanyl-3)uracil of the formula (I):

stimulating protective activity of phagocytes.

The specified connection and its properties are not described in literature.

The claimed compound synthesized by the interaction of 6-methyluracil, 2-chloromethylstyrene in the presence of potassium hydroxide in aqueous medium in tiirn-titanoboa rearrangement.

Example 1. The synthesis of the claimed compounds

To the solution was 4.02 g (72 mmol) of potassium hydroxide in 60 ml of water add 7,56 g (60 mmol) of 6-methyluracil and heated to 50°C. the ZAT what type of 6.9 g (66 mmol) of 2-chloromethylstyrene and stirred for 2 hours at 50-55°C. The precipitate is filtered from the hot reaction mixture is treated with ethyl acetate, hot water, dried at 60°C. MP.=231-233°C. Obtain 3.03 g (29%) of 6-methyl-1-(titanyl-3)uracil, purify by crystallization from an ethanol water mixture (volume ratio 1:1). Neproreagirovavshimi 6-methyluracil quantitatively return in the synthesis.

IR spectrum, ν, cm-1: 710 (S(CH2)2), 1348 (C-N), 1741 (C2=O), 1640 (C4=O), 1607 (C=C), 2953 (N-H).

An NMR spectrum1H (DMFA-d7), δ, ppm: of 1.66 (3H, s, 6-CH3); 2,20 of-2.32 (2H, m, S(CH)2); 3,34 is 3.40 (2H, m, S(CH)2); 4,60 (1H, s, 5-H); 5,15-to 5.21 (1H, m, NCH); 10,30 (1H, ush. C, 3-NH).

An NMR spectrum13(DMFA-d7), δ, ppm: 17,99 (6-CH3); 32,07 (S(CH2)2); 47,05 (NCH); 151,95 (5); 152,45 (6); 162,39 (2); 162,59 (4).

Mass spectrum (ES, 70 eV), m/z (IRel,%): 198 [M]+(28), 151 [M-SMe]+(17), 127 [M-CHS(CH2)2]+(100).

Elemental analysis.

Found, %: C 48,51; H 5,15; N 14,58 - C8H10O2N2S.

Calculated, %: C 48,55; N To 5.21; N 14,37.

The inventive compound is a white or white with a yellowish sheen crystalline powder, insoluble in water, ethanol, chloroform, soluble in dimethylformamide, dimethylsulfoxide, alkali solutions.

Example 2. Phagocytic activity

The effect of the claimed compounds and drug comparisons on the processes of free radical oxidation (What About) in model systems in vitro was studied using a rapid method, registration-based chemiluminescence (CHL) fluorescence arising from the interaction of free radicals (Baimatov V.N., Farkhutdinov P.P., Bagautdinov A.M. // Chemiluminescent methods for the study of free radical oxidation in agriculture, veterinary medicine and animal husbandry. - Ufa, Izd-vo "Health of Bashkortostan", 2009. - 104 S.).

The chemiluminescence was detected on the installation HLM-003 (Russia). Chlorophyll model systems were characterized by spontaneous light emission, quick flash and then developing a slow flash. The main most informative characteristics of CHL serve sutasoma glow determined by the intensity of the radiation, and the maximum amplitude of the glow.

To assess the impact of these compounds on the processes SRO in vitro studies were carried out on model systems that generate reactive oxygen species (ROS) in blood cells (model of phagocytosis).

The impacts on the processes of generation of free radicals by phagocytes was studied according to the scheme: heparinized venous blood in a volume of 0.1 ml were incubated with study drug for 5 min, then mixed with 2.0 ml of warmed up to 37°C of a solution lyuminola (5×10-5M) and measured CHL within 5 minutes

The drugs were added in model systems at concentrations relevant therapeutic e is ze prescribed drugs, - methyluracil. As control was used a model system in which instead of the investigated drugs were added to 0.9% saline in the same volume.

The invention is illustrated in the drawing, which shows the influence of the proposed connection and methyluracil on the processes SRO in the model system of phagocytosis (venous blood), where control, I declare the connection II is a drug comparison methyluracil.

In the blood the formation of ROS was accompanied by chemiluminescence, growing in the presence of lyuminola. The chemiluminescence intensity correlates with the oxygen and the degree of completion of phagocytosis. Adding the claimed compounds caused an increase in setosum and maximum luminosity Lomonosovskiy chemiluminescence compared to the level defined parameters of intact red blood cells (see drawing). This suggests that this compound stimulates the phagocytic activity of blood cells.

The influence of the proposed connection on the processes SRO in the model system of phagocytosis presented in the table.

The claimed chemical compound stimulates the phagocytic activity of blood cells, surpassing methyluracil 2 times.

Table
The influence of tawlae the CSOs connection on the processes SRO in the model system of phagocytosis
ConnectionBlood cells (sutasoma, cu) 0.01 mg/ml
Control43,6
I65,8
II131,0

1. 6-Methyl-1-(titanyl-3)uracil of the formula:

2. The substance according to claim 1, stimulating protective activity of phagocytes.



 

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20 cl, 5 ex, 4 tbl, 7 ex

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20 cl, 5 ex, 4 tbl, 7 ex

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4 ex

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30 cl, 3 ex

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