SU694020A1 - Esters of alpha,alpha-dimethyl-beta-triethylsiloxycarboxalic acids possessing antiinflammating activity and their preparation method - Google Patents

Description

a yy k with: o a

EH The compounds of formula 1 are colorless liquids with a faint odor, insoluble in water, well soluble in organic solvents. Investigation of the biological activity of the esters of OS, OS-dimethyl-triethylsiloxycarboxylic acids showed that they have an anti-inflammatory effect. The proposed compounds were tested for intraperitoneal administration of Wistar rats to white rats. For the evaluation of anti-inflammatory effects, a formalin inflammation model was used, for which, under the planktic aponeurosis of the hind paws

Table 2 introduced a 2.5% formalin solution in a volume of 0.1 ml. The magnitude of foot edema was determined by the L. S. Salmov's (1958) oncometric method 3 and 6 hours after the introduction of formalin. Test compounds were administered intraperitoneally at a dose of 80 mg / kg (1/10 of LDyo) in 0.5 hours and 3 hours after the phlogogenic agent: equi-volume amounts of 2 ° starch mucus were administered to the control group. compared with that of phenylbutazone. Studies have shown that oi, a-dimethyl-p-triethylsiloxycarboxylic acid esters have an anti-inflammatory effect. The data are given in table. 2

Methyl ether on. , o6-dimethyl- - triethyl- 80

siloxybutyric acid

Ethyl ester (X, c-dimethyl-triyethylsiloxycanoic acid

Control - starch mucus

Phenylbutazone (reference standard) P - calculated in comparison with phenylbutazone.

The proposed drugs have low toxicity, they exceed 800 mg / kg.

Thus, the claimed compounds are biologically active and can be used in practical medicine.

Claims (2)

1. Esters of Sch, SU.-dimethyl- (3-triethylsiloxycarboxylic acids ob51, 9 51.7 800 P 0.01 P 0.001 Pj 0.05  0.5 8055,957,5 Р 0,01 Р 1 - 0,001 Rg OD Р 0,5 118 79 2% 32 48 thirty formula 55 С1н-С (СНз) г-ЙООА1х RO LldzHsJs where r Sn C 7. . A1K -jH exhibiting anti-inflammatory activity. 2. A process for the preparation of compounds according to Claim 1, comprising: that the ester pi,: -dimethyl- / -carcinocontrol; P / 2 calculated in comparison with IHofoteii.t, the boranic acid is subjected to reaction with triethylsilane in the presence of zinc chloride as a catalyst at 105-110 ° C. .one l%.% 8 Sources of information taken into account during the examination 1. L.Birkofer, A. Ritter, N. Wieden. Veg. 1962, 95, p, 971.