1-(8-Bromo-2-methyl-4-thioxo-3,4,5,6-tetra-hydro-2H-2,6-methano-1,3-benzoxazocin-11-yl)ethanone.

In the title compound, C(14)H(14)BrNO(2)S, there are two similar non-equivalent mol-ecules in the asymmetric unit, displaying three chiral centres each. In the crystal structure, they are linked by inter-molecular N-H⋯O hydrogen bonds to form infinite chains, which are in turn connected by weak Br⋯H and S⋯H inter-actions.

Use of a complex approach for assessment of metamizole sodium and acetylsalicylic acid toxicity, genotoxicity and cytotoxicity.

A complex approach based on the use of test organisms belonging to different systematic groups (plants, invertebrates and vertebrates), as well as the nucleolar biomarker and the micronucleus test on their cells, was applied to assess the toxicity, cytotoxicity and genotoxicity of two pharmaceutical substances (metamizole sodium and acetylsalicylic acid) applied at ic(50) concentrations for mammalian cells. The compound acetylsalicylic acid was evaluated at a concentration (1.6 x 10(3) mg l(-1)) that was non-toxic for bioassays based on fish (Carassius auratus gibelio) and hydra (Hydra attenuata) and acutely toxic for bioassays with ceriodaphnia (Ceriodaphnia affinis) and onion (Allium cepa). The metamizole sodium solution (6.25%) demonstrated acute toxicity for the whole set of test organisms. Both drugs, after their 30-360 min influence on the test organisms, first changed the nucleolar size in plant and animal cells (i.e. the transcriptional activity of ribosomal genes was affected most significantly). Moreover, the metamizole sodium solution caused nucleolar structural damage in 90% of hydra cells as early as after 30 min of exposure. The acetylsalicylic acid solution inhibited essentially the rate of cell division in the meristem of onion roots (the mitotic index decreased to 9.6 per thousand, as compared 51.7 per thousand for the control). The carp incubation and the onion germination in the acetylsalicylic acid solution showed a reproducible increase in the frequency of cells with micronuclei (2 and 5.5 times, respectively) and double nuclei (3 and 1.5 times, respectively). The approach described herein may be applied for obtaining rapid, cost-efficient and useful supplementary data on different types of toxicity for marketed drugs as well as for drugs under development.

[The physiological properties of the action of a new analgesic and antipyretic preparation]. / Fiziolohichni vlastyvosti diï novoho anal'getychnoho i zharoznyzhuval'noho preparatu.

Children's morbidity from Chernobyl accident aftereffects was studied. New preparation "Paravit" was created. This preparation is for treatment illnesses, which are accompanied by pain and slight temperature. Tablets "Paravit" have mark, which allows exact dosing for children of different age. The specific pharmacological investigation of "Paravit" were taken. They showed that new preparation possesses active antipyretic and analgetic properties.

[Radioprotective effect of a new pharmaceutical "glucosuccine"]. / Radioprotektornoe deistvie novogo farmakologicheskogo sredstva "gliukosuktsin".

The experiments on 6-Gy irradiated rats have revealed that the new biologically active substance. Glucosuccine has a radioprotective effect which depends upon the route of administration. The agent was demonstrated to produce a profound radioprotective rather than therapeutical effects. Its administration for 30 days proved to be less effective than its triple use prior to and following irradiation.

[Search for anti-inflammatory preparations among the derivatives of succinic acid heteryl amides]. / Poisk protivovospalitel'nykh preparatov v riadu proizvodnykh geterilamidov iantarnoi kisloty.

The antiinflammatory activity and acute toxicity of 44 derivatives of heteryl amides of succinic acid (acids, esters, amides) were studied. This series of compounds was found to be promising for the search of nonsteroidal, practically nontoxic antiphlogistics. The structural-pharmacological analysis was performed and the dependence of the biological effect on the compound structure was revealed.

[Search for cholagogic preparations in a series of heterylamide derivatives of ethylene (ethane) dicarboxylic acids]. / Poisk zhelchegonnykh preparatov v riadu proizvodnykh geterilamidov étilen(étan)-dikarbonovykh kislot.

Study of the choleretic activity of heterylamides of dicarboxylic acids has demonstrated that search for choleretic drugs in this series holds promise. The relationship of the choleretic activity and toxicity to the chemical structure of the compounds has been shown with special reference to 10 compounds--the derivatives of ethylene (ethane)-dicarboxylic acids. It has been discovered that the occurrence of the choleretic action is essentially determined by the presence in the structure of the compounds of a free cyrboxylic group. It has been also demonstrated that etherification or amidation of this group or hydrogenation of the unsaturated bond lead to the reduction or complete loss of the choleretic activity.

[Change in the anti-inflammatory activity of nonsteroidal antiphlogistics in conditions of acute hypoxic hypoxia]. / Izmenenie protivovospalitel'noi aktivnosti nesteroidnykh antiflogistikov v usloviiakh ostroi gipoksicheskoi gipoksii.

It has been shown on animals with experimental histamine edema under acute hypoxic hypoxia that anti-inflammatory properties of the known non-steroidal antiphlogistics and new derivatives of fumaric acid heterylamides administered in a dose of 10% of the LD50 underwent changes. At "altitudes" of 5000 and 10000 m a high enough anti-inflammatory activity was preserved by the drugs that, apart from an anti-exudative action, produced an antihypoxic one. The other non-steroidal anti-inflammatory drugs under study demonstrated either a lowered activity or completely lost it, depending on the "altitude".

[Hypoglycemic activity of aromatic sulfohydrazides and their derivatives]. / Gipoglikemicheskaia aktivnost' aromaticheskikh sul'fogidrazidov i ikh proizvodnykh.

Tests on rabbits revealed the aromatic sulfohydrazides and their derivatives to display hypoglycemic action. A number of compounds superior to butamide by their sugar-lowering action and of low toxicity were discovered. The relationship between the chemical structure of the study substances and their hypoglycemic action is discussed.