Abrasive tool making process – material – or composition
Patent
1988-04-04
1989-06-13
Springer, David B.
Abrasive tool making process, material, or composition
548550, C07D20724, A61K 3140
Patent
active
048393800
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE ART
The present invention relates to organic chemistry and, more particularly, to a novel compound, viz., 1-thiocarbamylmethylpyrrolidine-2-thione, and to a process for preparing same. Said compound exhibits antihypoxic and nootropic activity.
PRIOR ART
Known in the art are different compounds exhibiting antihypoxic and nootropic activity, for instance, 1-carbamidomethylpyrrolidone-2 of the formula ##STR3## which is an active principle of the pharamcological preparation pyracetam (cf. Mashkovsky M. D., Roshcina L. F., Polezhaeva A. I., "Some Specific Features of Pharmacological Action of Pyracetam", Farmakologia i Toksikologia, No. 6, 1977, pp. 676-684).
Pyracetam is the main representative of a novel class of pharmacologically active compounds-nootropics, whose main pharmacological characteristics reside in producing a protective effect in various forms of oyxgen deficiency (antihypoxic effect) and a positive effect on the processes of learning and memory.
Pyracetam exhibits nootropic activity only when used in high doses: from 500 to 2000 mg/kg.
Furthermore, pyracetam is characterized by the absence of a pronounced stimulative effect on the mechanisms of memory consolidation and performance of conditioned reflexes.
DISCLOSURE OF THE INVENTION
The compound of the present invention is novel and has not been described in the literature.
The present invention is directed to the provision of a novel compound possessing simultaneously an increased antihypoxic and nootropic activity and a low toxicity.
This object is accomplished due to the fact that the novel compound, 1-thiocarbamylmethylpyrrolidine-2-thione, according to the invention, has the following formula: ##STR4##
The compound of the invention is a crystalline substance, soluble in N,N-dimethylformamide, crystallizing from water, alcohols, ethylacetate, chloroform, benzene, acetaone, insoluble in ether, hexane, stable in storage, m.p. 156.degree.-158.degree. C. (from isopropanol).
The structure of the compound has been identified by the data of elemental analysis; IR spectrum displaying bands at 1630, 3110, and 3260 cm.sup.-1 (NH.sub.2 -group) and 1120 cm.sup.-1 (C=S); mass spectrum comprising a peak of molecular ion 174 m/z, and according to which the compound comprises two atoms of sulphur.
Best Way of Carrying the Invention into Effect
The compound according to the present invention has been tested for antihypoxic and nootropic activity in experiments on animals.
The antihypoxic effect of the compound according to the present invention was studied in comparison with pyracetam on various experimental models of hypoxic states in experiments on mice and rats. The compound according to the present invention and pyracetam were administered intraperitoneally in the form of an aqueous emulsion prepared with Tween-80.
Tests were carried out on a model of an acute hypoxic hypoxia with hypercapnia.
The tests were conducted using 540 nondescript while male mice with a mass of 20-22 g. Each mouse was separately placed into a sealed chamber (with the capacity of 250 ml) 60 minutes after administration of the compound according to the present invention in the doses of 50, 100, 250, 500 and 750 mg/kg. The control animals were issued with an isotonic solution of sodium chloride. The antihypoxic activity was assessed by the lifespan of the mice in the sealed chamber (in minutes).
The results of the study of antihypoxic effect of the compound according to the present invention in comparison with the prior art preparation--pyracetam--are given in Table 1 hereinbelow.
As it is seen from the experimental data given in Table 1, the compound according to the present invention extended, as compared to the control, the mice lifespan under conditions of an acute hypoxic hypoxia by about 2 times already at the dose of 100 mg/kg, whereas at the dose of 750 kmg/kg--by 4 times (324.5% increase) which demonstrates its high antihypoxic activity. In its antihypoxic effect the compound according to the present invention is considerably superior to pyracetam.
Bobkov Jury G.
Glushkov Robert G.
Granik Vladimir G.
Ivanova Irina A.
Losev Alexandr S.
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