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PubMed1995

Synthesis and pharmacological activities of novel bicyclic thiazoline derivatives as hepatoprotective agents. I. 8-Ethoxycarbonyl-5,6-dihydrothiazolo[2,3-c][1,4]thiazine derivatives.

A series of bicyclic thiazoline derivatives (4a-s) was synthesized and evaluated for hepatoprotective activity against galactosamine-induced and monoclonal antibody-induced acute liver injuries in rats. The structure-activity relationships were investigated. Among the compounds synthesized, ethyl 3-(N-methylcarbamoyl)-5,6-dihydrothiazolo[2,3-c][1,4]thiazin e-8- carboxylate (4p) exhibited remarkable hepatoprotective activity and lower toxicity. This compound suppressed galactosamine-induced hepatic injury at 100 mg/kg by gavage and further prevented monoclonal antibody-induced hepatic injury at 30 mg/kg by intraperitoneal injection, as evaluated by measuring changes in serum transaminase activities.

Animals↗
PubMed1986

Cardiovascular effects of ZSY-27 [5-methyl-6-(4-pyridinyl)-2H-1,4-thiazine-3(4H)-one X hydrochloride] in the dog cross-circulated atrial preparation.

A new cardiotonic compound, 5-methyl-6-(4-pyridinyl)-2H-1,4-thiazine-3(4H)-one X hydrochloride (ZSY-27), was investigated in cross-circulated dog atrial muscle preparations. When ZSY-27 was intravenously administered to the donor dog, a dose-dependent depressor effect with slight sinus tachycardia was induced in the donor dog. At the same time, a significant dose-dependent increase in developed tension was usually observed in an isolated atrium perfused with donor's arterial blood, but there were no significant changes in sinus cycle length and sinoatrial conduction time. The ZSY-27-induced positive inotropic effect was not significantly influenced by treatment with propranolol in doses which completely inhibited norepinephrine-induced positive chronotropic and inotropic effects. When ZSY-27 was injected into the cannulated sinus node artery of the isolated atrium, dose dependent positive chronotropic and inotropic effects were induced. The dominant increases in developed tension by ZSY-27 were similar to effects of other phosphodiesterase inhibitors, such as papaverine and aminophylline. From these results, it is concluded that ZSY-27 has non-adrenergic, cardiotonic properties with a depressor effect.

Aminophylline↗
PubMed1975

Metal contaminants in commercial thiazine dyes.

The iron, potassium, sodium and zinc content of commercial samples of the thiazine dyes azure A (C.I. 52005), azure B (C.I. 52010), azure C (C.I. 52002), methylene blue (C.I. 52015), new methylene blue (C.I. 52030), polychrome methylene blue, thionine (C.I. 52000) and toluidine blue (C.I. 52040) have been determined by atomic absorption spectrophotometry. The metal concentration varied widely in the 38 samples examined--iron, potassium, sodium and zinc together comprised between 0.02% and 25.35% of individual samples.

Chromatography, Ion Exchange↗
PubMedDate not supplied

Synthesis and fungicidal activity of substituted pyrazolo[5,4-b] pyridine/pyrid-6-ones and pyrazolo[5,4-d]thiazines.

6-amino-1-Aryloxyaceto-4-aryl-5-cyano-4,5-dihydro-3-methy-l-1H-pyrazolo [5,4-b] pyridines (3)/pyrid-6-ones (4) and 1-Aryloxyaceto-6-amino-4-aryl-3-methyl-4H-pyrazolo[5,4-d]-1,3-thiazines (5), have been prepared by Michael addition between a,b-unsaturated ketones (2) and malononitrile/ethyl cyanoacetate and thiourea respectively. The antifungal activity against Aspergillus niger, Helminthosporium oryzae and Pyricularia oryzae have been evaluated and compared with commercial fungicide Carbendazim tested under similar conditions.

Antifungal Agents↗
PubMed1992

Synthesis, structure and biological activity of 1,2,4-triazolo-1,3-thiazine derivatives.

A group of condensed triazole-thiazine derivatives (2a-i, 3b, 3j) was obtained in reaction of the corresponding 5-substituted 1,2,4-triazole-3-thiones (1a-j) with epichlorohydrin in alkaline medium. The structure of the compounds synthesized was confirmed by spectral and roentgenographic methods. Tuberculostatic and circulatory activities of the compounds were also studied.

Animals↗
PubMed2006

Synthesis and biological evaluation of some pyrimidine, pyrimido[2,1-b][1,3]thiazine and thiazolo[3,2-a]pyrimidine derivatives.

4,6-Diamino-1H-pyrimidine-2-thione (1) was used for the preparation of pyrimidine derivatives 2-5. Compound 5 was cyclized to produce pyrimido[2,1-b][1,3]thiazine derivative 6 which was condensed with p-chlorobenzaldehyde to give compound 7. The latter compound was reacted with hydroxylamine to give isoxazolo[4,5-d]thiazino[2,3-a]pyrimidine 8. Compound 8b was treated with 2-chloroethyl methyl ether to afford compound 9. Similarly, compound 3 reacted with chloroacetic acid to give thiazolo[3,2-a]pyrimidine 10, which was condensed with p-chlorobenzaldehyde to give compound 11. Compound 11 was condensed with hydroxylamine to give isoxazolo[4,5-d]thiazolo[2,3-a]pyrimidine 12. Compound 12b was treated with 2-chloroethyl methyl ether to afford compound 13. Biological evaluation of some prepared products showed that many of them revealed promising antimicrobial activity.

Anti-Infective Agents↗
PubMedDate not supplied

Synthesis and biological activity of pyrimido[2,1-b][1,3]thiazine, [1,3]thiazino[3,2-a]purine and [1,2,3]triazolo[4,5-d][1,3]thiazino[3,2-a]pyrimidine derivatives and thiazole analogues.

Some series of thiazolo[3,2-a]pyrimidine, pyrimido[2,1-b] [1,3]thiazine, thiazolo[3,2-a]purine, [1,3]thiazino[3,2-a]purine, thiazolo[3,2-a][1,2,3]triazolo[4,5-d]pyrimidine and [1,2,3]triazolo[4,5-d][1,3]thiazino[3,2-a]pyrimidine derivatives, variously functionalized, were prepared. The compounds were tested for antimicrobial and antimycotic activity on a number of strains, namely: E. coli, Proteus vulgaris, P. mirabilis, Pseudomonas aeruginosa, Salmonella sp., Staphylococcus aureus, S. faecalis, Bacillus subtilis, Sarcina lutea, Candida albicans, C. tropicalis, Aspergillus sp., and for antiviral activity on Herpes simplex virus Type 1, Vesicular stomatitis virus and Coxsackievirus B5. The compounds proved to be devoid of activity against viruses and gram-negative bacteria, while some of them exhibited modest activity against gram-positive bacterial strains.

Anti-Bacterial Agents↗
PubMed1989

The influence of cationic thiazine dyes on eosin Y-uptake of red blood cells in Romanowsky-Giemsa type stains.

In the present study we have investigated the uptake of cationic thiazine dyes and of the anionic Eosin Y by red blood cells (RBCs). Blood smears were stained with Azure B-Eosin Y, Methylene Blue-Eosin Y, Thionin-Eosin Y and with the cationic and anionic dyes alone at varying concentrations. Dye content of erythrocytes was measured with a Vickers M 85a microdensitometer. Nuclear chromatin features of white blood cells were investigated with the IBAS 2000 image analyser. Azure B favoured Eosin Y uptake of RBCs remarkably, and vice versa. There was no clear indication of that type of molecular interaction which characterizes the generation of the colour purple on polyanions. Methylene Blue and Thionin left Eosin Y uptake unaffected, but contamination of the standard Azure B-Eosin Y stain with Methylene Blue obviously affected Azure B-Eosin Y uptake, probably by competition of Methylene Blue and Azure B binding in RBCs. Furthermore, Methylene Blue contamination of the standard stain increased the rate of error in image analysis of white blood cell nuclei due to variations of staining intensity. For cytophotometry and image analysis of blood smears the standard Azure B-Eosin Y stain is by far superior to the commercial stain which normally is contaminated with Methylene Blue and some of the lower azures.

Azure Stains↗
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

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↗
PubMedDate not supplied

[Toxicity and radioprotective properties of 1,3-oxazine and 1,3-thiazine derivatives].

Toxicity and radioprotective properties of 18 derivatives of oxazine and thiazine with a varying degree of the cycle saturation were studied in experiments on mice. Monotypic regularity in variations of their toxic properties relative to the chemical structure was noted. 4,4,6-Trimethyl-2-dimethylamino-4H-1,3-oxazine exerted a pronounced radioprotective action.

Animals↗
PubMed1980

[Hydrogenated and cyclohomologous derivatives of phenothiazine. Synthesis and pharmacological activity of various cycloalkyl derivatives of 4H-benzo(b)(1,4)thiazine].

The synthesis and the results of pharmacological screening of 4H-benzo[b][1,4]thiazine derivatives are described. These substances were prepared by reacting 2,2'-dithiodianiline with ethyl-2-oxocycloalkanecarboxylates followed by NaBH4 reduction. The pharmacological results indicate remarkable depressive activity [see (IV b) (n = 3)] shown by 100% potentiation of barbituric-induced sleeping time.

Animals↗
PubMedDate not supplied

[Radiation-induced binding of 2-amino-5,6-dihydro-1,3-4H-thiazine to DNA].

A study was made of the nature of radiation--induced bonds between DNA and 2-amino-5,6-dehydro-4H-thiazine (2-ADT) having a radioprotective action. Using the gelfiltration method and 35S-2-ADT, it was shown that the amount of the radioprotector bound to DNA increased with radiation dose and did not depend on the postirradiation treatment with 3 M LiCl or 3 M urea. No marked binding was noted after mixing the separately exposed DNA and the protector. It is concluded that a covalent linkage of DNA and 2-ADT occurs, upon irradiation, via short-living states of DNA and (or) the protector.

Cobalt Radioisotopes↗
PubMedDate not supplied

[Antithyroid activity of various newly synthesized 1,3-thiazine derivatives].

Experiments were performed on rats. It was revealed that three newly-synthesized 1,3-thiazine derivative (1,3-thiazandithion-2,4, 1,3-thiazanthion-2-on-4-thiosemicarbazone-4, and 1,3-thiazandion-2,4) possessed and antithyroidal action in doses equal to 15% of LD50; in the two former preparations it was accompanied by an goiterogenic effect. 1,3-thiazandion-2,4 had the most antithyroidal action and relatively weak goiterogenic effect.

Animals↗
PubMed1995

Synthesis and pharmacological study of some derivatives of pyrazolo[4,3-c]pyrido[3,2-c]-1,2-thiazine-5,5-dioxide, a novel heterocyclic ring system.

Starting from pyridothiazines 1 and N-methyl(phenyl)hydrazines isomeric derivatives 2 and 3 of the pyrazolo[4,3-c]pyrido[3,2-e]-1,2-thiazine, a new heterocyclic ring system, have been obtained. The structure of the synthesized compounds was confirmed by spectroscopic and elemental analyses. The results of the preliminary pharmacological study of CNS effects caused by compounds 2 are reported.

Analgesics↗