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Enteral administration of oxymethyluracil in non-inbred albino rats decreased the inflammatory reaction to histamine, serotonin, bradykinin, carrageenan and trypsin, (being similar to voltaren) and reduced granulomatous inflammation, but influenced the proliferation to a lower extent than did voltaren. In contrast to voltarcen, oxymethyluracil also exhibited gastroprotective antiulcer properties.

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Hemisuccinates, hemiphthalates, acetylsalicylates, cinnamates, and p-methoxycinnamates of lupeol, betulin, and 3-O-acetylbetulin were synthesized via interaction with corresponding acid anhydrides or acid chlorides. A number of betulin esters in position 3 and 28 were shown to exhibit a pronounced hepatoprotective effect similar to that of betulin and silibor. These experimental data were in a good agreement with the computer prediction of their biological activity. Betulin 3,28-bis-hemiphthalate was more effective than carsil in models of experimental hepatitis caused by carbon tetrachloride, tetracycline, and ethanol.

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In experimental study of antiulcerative activity of dibunol on various models of gastric ulcers in rats the drug caused a marked antiulcerative effect in all of them, reduced the incidence of ulcer formation, and shortened the time of ulcer healing. In a model of "acetic" ulcer dibunol oil solution led to quick normalization of lipid peroxidation in the gastric mucosa, which was evidence of high antioxidant activity in cases of ulcer lesions.

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Experiments on albino rats showed that pyrimidine derivatives reduce hemorrhagic damage of the gastric mucosa caused by indomethacin, acetylsalicylic acid, and ortophen. The derivatives of pyrimidine prevent the decrease in total acid phosphatase activity, increase alkaline phosphatase, and reduce the activity of lactate dehydrogenase.

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Pyrimidine derivatives increased the antibiotic therapy efficacy in albino rats irradiated with RUM-7 apparatus for close-focus roentgenotherapy. 2-Methyl-4-amino-6-oxypyrimidine was twice as efficient as oxymethyluracil and 6 times as efficient as methyluracil in the stimulation of the skin reparative regeneration. When the total irradiation was performed with LUCH-1 apparatus in a dose of 6 Gy the pyrimidine derivatives also increased the antibiotic therapy efficacy. After the prophylactic use of the pyrimidine derivatives for 7 days prior to the total irradiation their therapeutic effect increased, the level of the exudative component lowered, the tissue epithelization increased, the terms of the wound healing decreased and the animal lifespan increased.

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It was shown on noninbred albino rats with various affections of the skin that pyrimidine derivatives stimulated the skin reparative regeneration and increased the efficacy of antibiotic therapy of Staphylococcus and Proteus infected wounds. The therapeutic effect of 2-methyl-4-amino-6-oxypyrimidine was much higher than that of oxymethyluracil or methyluracil. The pyrimidine derivatives proved to be universal accelerators for reparative regeneration, were compatible with antibiotics and increased their efficacy.

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Triterpene 2-deoxy-alpha-D-hexopyranosides were synthesized by the glycosylation of oleanane triterpene alcohols with D-glucal and D-galactal acetates in the presence of di(sym-collidine)iodonium perchlorate with subsequent deiodination and deacetylation of the resulting 2-deoxy-2-iodo-alpha-D-glycosides. 2-Deoxy-alpha-D-arabino- and -lyxo-hexopyranosides of methyl glycyrrhetinate demonstrated pronounced antiulcer activity and stimulated reparative skin regeneration in rats more effectively than glycyrrhizic acid and methyluracil.

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The effect of the immunomodulator 2-methyl-4-amino-6-oxypyrimidine (MAOP)on delayed hypersensitivity was studied in experiments on mongrel mice and in C57Bl and CBA mice. The effect of MAOP and that of oxymethyluracil on delayed hypersensitivity to sheep erythrocytes and dinitrofluorobenzene were compared. Immunosuppression of mice was induced by hydrocortisone in a dose of 50 mg/kg.

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Triterpene 2,6-dideoxy-alpha-L-arabino-hexopyranosides were synthesized by the glycosylation of oleanane triterpene alcohols with L-rhamnal acetate in the presence of cationite KU-2-8 and lithium bromide. 2,6-Dideoxy-alpha-L-arabino-hexopyranosides of allobetulin and methyl glycyrrhetinate showed pronounced antiulcerous activity; the latter also stimulated reparative skin regeneration in rats and was effective as a hepatoprotectant.

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White mongrel mice (150 specimens) were used to study the effect of 2-methyl-4-amine-6-oxypyrimidine (MAOP) on the absorption capacity of reticulo-endothelial system (RES) compared to the oxymethyluracil. It was demonstrated that the MAOP stimulates much greater the absorption capacity of RES in different functional states than the oxymethyluracil.

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The experiments on mice with Staphylococcus infection at the background of immune suppression due to the treatment with prednisolone or imuran showed that the use of 2-methyl-4-amino-6-oxypyrimidine, a derivative of pyrimidine, increased the animal survival, their lifespan and the efficacy of the tobramycin therapy.

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The experiments on mice showed that some derivatives of pyrimidine i.e. 2-methyl-6-amino-6-oxypyrimidine and oxymisin increased the levomycetin efficacy in the treatment of experimental infections. The effect of 2-methyl-6-amino-6-oxypyrimidine proved to be higher in comparison to that of oxymethyluracil.

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The luteotropic and luteolytic properties of synthetic analogues of 11-desoxy-PGE1 were studied. Compounds Nos. 1 and 2 depending on the dose exerted the opposite effect: in low doses--luteotropic, in high doses--luteolytic. Compounds Nos. 3, 4 and 5 in the whole range of doses exhibited only luteolytic properties. The ranges of doses of prostaglandin exerting the luteotropic effect depend on the structural modifications of prostaglandin molecule. The luteolytic effect of synthetic analogue No. 5 was suggested to be determined by its influence on the hypophysis through the change of contents of cyclic nucleotides and gonadotropic hormones. It was demonstrated that the luteolytic effect of compound No. 5 is realized through the central nervous system, in particular, through the hypophysis.

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The pharmacological properties of 4 derivatives of 11-desoxy-prostaglandins E (uterotonic, luteolytic, hypotensive, anti-inflammatory, diarrhogenic ones and also acute toxicity) were studied. Compound I possessed the uterotonic activity which decreased with an alpha-chain elongation and a radical introduction into a benzene ring. Compounds I and II exhibited the luteotropic properties at low doses and the luteolytic ones at high doses. The compounds under study had the hypotensive activity due to the presence of a benzene ring in a W-chain.

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Experiments were carried out on 150 male rats weighing 200-250 g and 42 white mice weighing 18-20 g by using two models of acute pancreatitis, two models of inflammation and studying osmotic resistance of erythrocytes. In experimental pancreatitis hydroxymethyluracil (50 mg/kg) decreased the blood lipase activity. The therapeutic effect of the agent is related to its anti-inflammatory and membrane-protecting properties.

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The results of studies on the biological activity of seven synthetic analogues of prostaglandins are presented. All the analogues under study possess uterotonic, antiulcer and anti-inflammatory activity; all the compounds except S1 induce diarrhea. The synthetic analogues studied decrease transiently and slightly the arterial blood pressure.

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