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Biomedical subjects

T Jakóbiec

Publications and source records attributed to T Jakóbiec.

At least 19 recordsLinked to original sources
PubMed1984

Investigations on derivatives of 5-aminomethyl-6-/p-chloro-phenyl/-4, 5-dihydro-2H-pyridazin-3-one.

Several new derivatives of 5-aminomethyl-6-/p-chlorophenyl/-4, 5-dihydro-2H-pyridazin-3-one have been obtained. The substrates, beta-aminomethyl-beta-/p-chlorobenzoyl/-propionic acid derivatives 1-5, were converted by reactions with hydrazine hydrate or monosubstituted hydrazines, i.e. phenylhydrazine and N-/beta-hydroxyethyl/-hydrazine into appropriate derivatives of 5-aminomethyl-6-/p-chlorophenyl/-4,5-dihydro-2H-pyridazin-3-one 6-18. Compounds 7, 8, 11, 12, 14, 15, and 18 show depressant activity on CNS, while compounds 7a, 9a, 10, 11, 14, 15 possess cytostatic and immunosuppressive activities.

Animals↗
PubMed1984

New 2-substituted derivatives of 5-aminomethyl-6-/p-chlorophenyl/-4,5-dihydro-2H-pyridazin-3-one.

Several new 2-substituted derivatives of 5-aminomethyl-6-/p-chlorophenyl/-4,5-dihydro-2H-pyridazin-3-one were synthesized. The derivatives of 5-aminomethyl-6-/p-chlorophenyl/-4,5-dihydro-2H-pyridazin-3-one (1-4) were used as the substrates. These compounds were converted by the reactions of cyanoethylation, hydroxymethylation and aminomethylation into appropriate 2-substituted derivatives of 5-aminomethyl-6-/p-chlorophenyl/-4,5-dihydro-2H-pyridazin-3-one (5-28). Some of these compounds (5, 9 and 16) show anticonvulsant activity, while compounds 6, 7, 11-13 and 20 possess immunosuppressive activity.

Animals↗
PubMed1982

Synthesis of D,L beta-aminomethyl derivatives of gamma-(p-chlorophenyl)-tetrahydrofuran-2-one.

Several new D,L beta-aminomethyl derivatives of gamma-(p-chlorophenyl)-tetrahydrofuran-2-one have been synthesized. The derivatives of D,L beta-aminomethyl-beta-(p-chlorobenzoyl)-propionic acid 2-6 were used as the substrates. These compounds were obtained by the Mannich reaction from acid 1, cyclic secondary amines and formaldehyde. After the reduction with NaBH4, and cyclization, derivatives 2-6 were converted into the appropriate derivatives of tetrahydrofuran-2-one 9-13. Some of the obtained compounds (5, 6, 8, 11 and 12) showed depressant activity against the central nervous system.

Animals↗
PubMed1982

Synthesis of derivatives of beta-aminomethyl-gamma-(p-chlorophenyl)-gamma-hydroxybutyric acid.

Several new derivatives of beta-aminomethyl-gamma-(p-chlorophenyl)-gamma-hydroxybutyric acids have been obtained. The substrates, beta-aminomethyl derivatives of gamma-(p-chlorophenyl)-tetrahydrofuranone-2 1-4, were converted by the reactions of ammonolysis, aminolysis and hydrazinolysis into appropriate amides and hydrazides of beta-aminomethyl-gamma-(p-chlorophenyl)-gamma-hydroxybutyric acid. Compounds 10, 11, 16, 18, 19 and 20 show depressant activity on CNS, while compounds 6 and 8 demonstrate antiinflammatory action.

Animals↗
PubMed1981

Syntheses and pharmacological analysis of new derivatives of tetrahydro-[1,3]-thiazine and 2-thiobarbituric acid.

Three groups of compounds:1,3-thiazine derivatives, 2-thiobarbituric acid derivatives and noncyclic thioureide were obtained as a result of condensation of some N, N1-derivatives of thiocarbamide and malonyl dichlorides, depending on the reaction conditions and chemical character of reagents. It was observed that the substituents beside nitrogen atoms of thiocarbamides, the kind of acid chloride and reaction conditions influenced the course of reaction. The structure of the newly synthesized compounds was proved by the analysis of PMR spectrum and the interpretation of IR spectrum. In the performed pharmacological examination immunotropic and anti-inflammatory activity of these compounds was determined. Among 1,3-thiazine derivatives, 5,5-diallyl-2-phenylimino-3-phenyl-2,3,4,5-tetrahydro-[1,3]-thiazine-4,6-dione and 5,5-diethyl-2-phenylimino-3-naphtyl-2,3,4,5-tetrahydro-[1,3]-thiazine-4,6-dione exhibited anti-inflammatory activity. The compounds also contained the immunotropic component, either stimulatory or suppressive, 2-thiobarbituric acid derivatives displayed stronger anti-inflammatory activity correlated mostly with the immunosuppressive activity. Some interdependence between chemical structure and biological activity in the group of the investigated 1,3-thiazines and 2-thiobarbituric acid derivatives was observed.

Animals↗
PubMed1981

Studies on derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid. IV. Addition reactions of thioglycolic acid to 2-N-aralkylidene derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

In the course of studies on compounds with expected antiinflammatory and immunosuppressive activity a series of new derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid have been synthesized. Several new and unexpected details of the chemical properties of these compounds were revealed. The chemical structure of the new compounds was confirmed by degradation and identification of the decomposition products and by spectral analysis.

Amino Acids↗
PubMed1981

Studies on derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid. V. Syntheses of 2-N-aralkylidene and 2-N-aralkyl derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

A number of new N-aralkylidene and N-aralkyl derivatives of amides and hydrazides of 2-amino-4-p-chlorophenylthiazole-5-acetic acid (III-XXIX) have been synthesized. These compounds were obtained in two various ways depending on the character of substituents in the carboxyl group. The chemical structure of the newly obtained compounds was determined on the basis of the data of elementary and spectral analyses.

Amino Acids↗
PubMed1981

Studies on derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid. VI. Syntheses and properties of 2-N-aralkyl-alpha-sulphoderivatives of tert-amides of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

In the course of the studies on compounds with expected antiinflammatory and immunosuppressive activity several new tert-amides derivatives of 2-N-aralkylamino-alpha-sulpho-2-amino-4-p-chlorophenylthiazole-5-acetic acid were synthesized. Some of the previously described Schiff bases reacted with aqueous alcoholic solution of sodium bisulphite and as a result several (III-VIII) alpha-sulphoderivatives were obtained. The course of the reactions was studied and the structure of the new compounds was confirmed.

Amides↗
PubMed1979

Studies on the derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid. I. Syntheses and pharmacological analysis of acylderivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

A number of new acyl and imidoderivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid (II) and its methyl ester (VII) were synthesized. Methyl ester VII heated in benzene solution with acid anhydrides was transformed into adequate acyl derivatives (VIII, IX, X, XIII, XVI). Some of them (X, XIII, XVII) by heating with acetic anhydride underwent cyclization and were transformed into the imido derivatives (XI, XIV, XVIII). Compounds XI, XIV and XVI heated with diluted aqueous solution of sodium hydroxide underwent selective hydrolysis giving the respective dicarboxylic acids XII, XV, XVII. Pharmacological analysis revealed that some of the synthesized preparations exert an anti-inflammatory effect and allow to draw limited relations between chemical structure and pharmacological activity in this group of compounds.

Analgesia↗
PubMed1979

Studies on the derivatives of thiazole acetic acid. II. Syntheses and pharmacological analysis of 2-N-aralkylidene and 2-N-aralkyl derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

A number of 2-N-aralkylidene, 2-N-aralkyl and 2-N-aralkyl-alpha-sulphoderivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid (I, R = H) and its methyl ester (I, R = CH3) were synthesized. As a result of condensation of methyl ester I with various aromatic aldehydes in boiling benzene solution, the Schiff-bases (anils) II--VIII were obtained. After reduction with NaBH4 compounds II--VIII were transformed into adequate amino esters IX--XV. Esters IX--XV heated with diluted aqueous solution of sodium hydroxide underwent selective hydrolysis giving the respective amino acids XVI--XXII. Some of Schiff bases (II, III, V, VII, VIII) reacted with aqueous alcoholic solution of sodium bisulphite after its several (XXIII--XXVII). alpha-sulphoderivatives had been obtained. Several tests were performed in order to detect the anti-inflammatory and immunosuppressive activity of the compounds. The pharmacological analysis allowed us to draw conclusions concerning the relationship between chemical structure and biological activity in this group of compounds. The most efficacious immunosuppressive and anti-inflammatory activity exhibited 2-aralkyl-alpha-sulphoderivatives.

Adjuvants, Immunologic↗
PubMed1978

Synthesis of derivatives of 2-amino-4-p-chlorophenylthiazole-5-acetic acid.

In the course of studies on compounds with expected antiinflammatory and immunosuppressive action a number of new derivatives of 2-amino-4-p-chlorophenylthiazole-s-acetic acid have been synthetized. The chemical structure of these compounds has been confirmed by elemental analysis and IR spectra. The newly obtained compounds were investigated pharmacologically. It has been found that some of the derivatives possess antiinflammatory and immunosuppressive activity.

Amino Acids↗
PubMed1978

Studies on derivatives of tetrahydro [1,3]-thiazine.

In the course of studies on compounds with expected antiinflammatory and immunosuppressive activity a series of new derivatives of tetrahydro [1,3]-thiazine-4-one-6-carboxylic acid, tetrahydro [1,3]-thiazine-4,6-dione and 2-thiobarbituric acid have been synthetized. Several new and unexpected details of the chemical behavior of these compounds were revealed. The chemical structure of the new compounds was confirmed by degradation and identification of the decomposition products and spectral analysis. Pharmacologic analysis showed that some of the compounds exerted an antiinflammatory and immunosuppressive activity.

Anti-Inflammatory Agents↗
PubMed1977

Studies on derivatives of phenyltetrahydrofuranone-2-carboxylic acids. VI. Derivatives of beta-phenyltetrahydrofuranone-2-beta-carboxylic acid.

Proceeding with the studies on derivatives of pheyl-tetrahydrofuranone-2-carboxylic acids the authors have stated that the reaction of hydroxymethylation of ethyl ester of beta-phenyl-beta-cyanopropionic acid I gives transitionally beta-phenyl-beta-cyano-beta-hydroxymethylpropionic acid II which, after a long time, transforms into an amide of beta-phenyl-tetrahydrofuranone-2-beta-carboxylic acid (III). Amide III is tranformed, through acid IV, into acid chloride V that gives a number of derivatives: amide III, substituted amides (VI-IX), methyl ester X, ureide XI, and aminomethylamides (XII, XIII). The chemical structure of these compounds has been confirmed by elemental analysis and IR and PMR spectra. The compounds newly obtained were invested pharmacologically. It has been found that some of the derivatives (III, VI, VII, VIII, XII, XIII) exert a depressing action on the central nervous system.

Central Nervous System↗