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T Zawisza

Publications and source records attributed to T Zawisza.

At least 19 recordsLinked to original sources
PubMed1990

Synthesis and properties of the derivatives of 2-alkylthio-4-oxo-3,4- (and -1,4)-dihydropyrido-[2,3-d]pyrimidine-5- and -6-carboxylic acids.

Condensation of diethyl 2-amino-6-methylpyridine-3,4-dicarboxylate (I) with the corresponding isothiocyanates afforded derivatives of ethyl 4-oxo-2-thioxo-1,2,3,4-tetrahydropyrido [2,3-d]pyrimidine-5-carboxylate (V-VII). Alkylation of (V), (VI) and (XI) gave the corresponding derivatives of ethyl 2-alkylthio-4-oxo-3,4-(and 1,4)-dihydropyrido[2,3-d]pyrimidine-5- and -6- carboxylate [(XII-XVI), (XX-XXII)]. Some of the obtained compounds were active pharmacologically.

Aggression↗
PubMed1989

Syntheses and properties of selected derivatives of pyrimido[5,4-e]-1,3-thiazine and pyrimido[4,5-d]pyrimidine.

In the reactions of ethyl 4-chloro/tosyloxy/-2-methylpyrimidine-5-carboxylate with differently substituted thioureas, new derivatives of 2,3-dihydro-7-methylpyrimido-[5,4-e]-1,3-thiazine (5-9) and of 7-methyl-1,2,3,4-tetrahydropyrimido[4,5-d]pyrimidine (12, 13) were obtained. Besides, some derivatives of 4-phenylamino-2-methylpyrimidine-5-carboxylic acid (15-20) were also synthesized. Structure of the compounds was confirmed by spectral analysis (IR, H-NMR) and chemical transformations. In the screening pharmacological examinations some of the compounds revealed analgesic, antiinflammatory and immunosuppressive activity.

Chemical Phenomena↗
PubMed1986

Synthesis and properties of amides of 1-benzyl-3-methyl- and 1-butyl-3-phenyl-7-methyl-4-oxo-2-thioxo (2,4-dioxo)-1,2,3,4-tetrahydropyrido-[2,3-d]pyrimidine-6-carboxy lic acids.

Amides of 1-benzyl-3,7-dimethyl-4-oxo-2-thioxo-1,2,3,4- tetrahydropyrido[2,3]pyrimidine-6-carboxylic acid were obtained by the condensation of ammonia, primary and secondary cyclic amines with the corresponding acid chloride. As by - products amides of 1-benzyl-3,7-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyr imidine-6- carboxylic acid were isolated as a result of desulfuration. The same reaction performed with chloride of 1-butyl-7-methyl-3-phenyl-4-oxo-2-thioxo-1,2,3,4-tetrahydropyri do[2,3- d]pyrimidine-6-carboxylic acid gave mainly the corresponding 2,4-dioxo-amides.

Analgesics↗
PubMed1986

A novel system: 2H-pyrido[3,2-e]-1,2-thiazine-1,1-dioxide. Synthesis and properties of some derivatives.

A rearrangement of 2H-2-acetonyl(phenacyl)-4,6-dimethyl- pyrido[3,2-d]isothiazoline-3-one-1,1-dioxides (I), (II) to derivatives of the unknown system of 2H-pyrido[3,2-e]-1,2-thiazine-1,1-dioxide (V), (XIII) is described; the synthesis of 2-N-substituted derivatives (VI - XII), (XIV - XVI) is also given. The structures of the new compounds were confirmed with elemental analyses and spectral data (I.R., N.M.R., MS). Some of the newly obtained compounds showed strong analgesic activity upon pharmacological screening.

Analgesics↗
PubMed1982

Investigations on the synthesis and properties of new derivatives of ethyl 3H-2-imino-7-methyl-4-oxopyrido [3,2-e]-1,3-thiazine-6-carboxylate and isomeric compounds.

Condensation of diethyl 2-chloro-6-methylpyridine-3,5-dicarboxylate (IV) with thiourea and alkyl or alkenyl N-mono- and N,N'-disubstituted thioureas gives mainly the corresponding derivatives of ethyl 3H-2-imino-7-methyl-4-oxopyrido [3,2-e]-1,3-thiazine-6-carboxylate (VI-XII). As by-products isomeric derivatives of ethyl 7-methyl-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrido [2,3-d) pyrimidine-6-carboxylate (XIII-XVIII) are formed.

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↗