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At least 19 recordsLinked to original sources
PubMed1978

Imidazo[1,2-a]-s-triazine nucleosides. Synthesis and antiviral activity of the N-bridgehead guanine, guanosine, and guanosine monophosphate analogues of imidazo[1,2-a]-s-triazine.

The first chemical synthesis of 2-aminoimidazo[1,2-a]-s-triazin-4-one (8), the corresponding nucleoside and nucleotide, and certain related derivatives of a new class of purine analogues containing a bridgehead nitrogen atom is described. Condensation of 2-amino-4-chloro-6-hydroxy-s-triazine (2) with aminoacetaldehyde dimethyl acetal followed by the ring annulation gave the guanine analogue 8. A similar ring annulation of 4-(2,2-dimethoxyethylamino)-s-triazine-2,6-dione (5) gave imidazo[1,2-a]-s-triazine-4,6-dione (9). Direct glycosylation of the trimethylsilyl derivative of 8 with 1-O-acetyl-2,3,5-tri-O-benzoyl-beta-D-ribofuranose in the presence of stannic chloride, followed by debenzoylation, gave the guanosine analogue 2-amino-8-(beta-D-ribofuranosyl)imidazo[1,2-a]-s-triazin-4-one (12b), which on deamination gave the xanthosine analogue 13. Phosphorylation of 12b gave 2-amino-8-(beta-D-ribofuranosyl)imidazo[1,2-a]-s-triazin-4-one 5'-monophosphate (II). The anomeric configuration has been determined unequivocally by using NMR of the 2',3'-O-isopropylidene derivate 10 and the site of ribosylation has been established by using 13C NMR spectroscopy. These compounds were tested against type 1 herpes, type 13 rhino, and type 3 parainfluenza viruses in tissue culture. Moderate rhinovirus activity was observed for several compounds at nontoxic dosage levels.

Antiviral Agents↗
PubMed1976

Pharmacological studies on triazine derivatives V Sedative and neuroleptic actions of 2-amino-4-[4-(2-hydroxyethyl)-piperazin-1-yl]-6-trifluoromethyl-s-triazine (TR-10).

Pharmacological properties of 2 amino-4-[4-(2-hydroxyethyl)-piperazin-1-yl]-6-trifluoromethyl-s-triazine (TR-10) were investigated in mice and rats. Chlorpromazine served as a reference compound. Tr-10 expressed in general the pharmacological profiles as neuroleptic ascertained by anti-methamphetamine activity, supression of conditioned avoidance response, taming effects, decrease in exploratory behavior and cataleptogenic activity. Among these effects, anti-methamphetamine action was most potent. Different from chlorpromazine, TR-10 showed a similar pharmacological activity pattern in the intraperitoneal and oral routes of administration as depicted from ED50/LD50 values. Although the effects relevant to neuroleptics were less potent than chlorpromazine, such were seen with TR-10 at lower doses than those causing muscle relaxation. TR-10 significantly depressed the spontaneous motor activity but showed no anti-convulsant action in mice. Hypothermic action, potentiating effects of hypnotics and alpha-adrenergic blocking action, characteristic to chlorpromazine, were very weak for TR-10. TR-10 also showed low toxicity in mice (LD50 = 820 mg/kg p.o., 465 mg/kg i.p.) compared with that of chlorpromazine (LD50 = 370 mg/kg p.o., 228 mg/kg i.p.).

Acetates↗
PubMed1979

Synthesis and antihypertensive activity of novel 3-hydrazino-5-phenyl-1,2,4-triazines.

In an effort to develop antihypertensive agents with peripheral vasodilator activity, a series of 40 novel 3-hydrazino-5-phenyl-1,2,4-triazines (II) were synthesized and evaluated in the spontaneously hypertensive rat assay (SHR assay). Based on the performance of the structurally related standard, hydralazine (I), 15 triazines were active. Thirteen of these hypotensive triazines possessed LD50 values in the mouse greater than I (LD50 = 100 mg/kg); only one active triazine had an LD50 value greater than 300 mg/kg (11d). Four asymmetric triazines had moderate antihypertensive activity and LD50 values greater than 300 mg/kg (6b, 7c, 8f, and 9g). Based on the relationship between toxicity and antihypertensive activity, three triazines (8f, 9g, and 11d) were chosen for dose-responses studies in the SHR assay. None were as efficacious as I, but all three were less toxic, resulting in similar therapeutic indices relative to I.

Animals↗
PubMed1979

Protein purification using immobilised triazine dyes.

This review attempts to identify proteins which selectively interact with immobilised triazine dyes such as Cibacron blue F3GA and Procion red HE 3B. Different support matrices are compared by examining the capacities of these dyes for proteins. Various approaches to the immobilisation of triazine dyes are considered together with the use of spacers. Some theories of the mechanism of protein retardation by immobilised dyes are discussed. A number of methods are suggested for the measurement of dye concentrations and for the modification of the binding of proteins to dye columns. The variety of elution methods is compared with a view to optimizing purifications. The scope of applications is reviewed as well as the choice of dye. Some advantages of triazine dyes over other affinity ligands are given. It is concluded that although no satisfactory mechanism for the binding of triazine dyes to proteins has yet been proposed, these dyes possess considerable potential for protein purification, particularly when applied on the large scale.

Animals↗
PubMed1977

A phase II study of triazinate (NSC 139105) in advanced colorectal carcinoma.

Triazinate (Baker's Antifol, NSC 139105) was given to 28 patients as a single agent in the chemotherapy of advanced colerectal carcinoma. The dosage utilized was 250 mg/m2 intravenously, administered daily in three consecutive days. Patients were evaluated at three weeks, six weeks, and then monthly until progression was evident. Various immunologic determinants (i.e., DNCB sensitization, immunoglobulins, recall skin tests, lymphocyte blastogenesis, and circulating lymphocytes, T-cells and B-cells) were obtained prior to treatment and at each re-evaluation. The principal side effects were dermatitis, stomatitis, diarrhea, nausea, somnolence, and leukopenia. There was no discernable effect of Triazinate on the immunologic determinants tested. There was one complete response, and four partial responses, for an objective regression rate of 18%. This study suggests that Triazinate has a definite, though limited, effect on advanced colorectal carcinoma.

Adenocarcinoma↗
PubMed1978

[Effect of 1,3,5-triazines on various bacteriophages and their hosts].

In the agar diffusion test 24 triazines were investigated with regard to their action on the mulplication of DNA phages (lambda and LPP-1) and RNA phages (M12 and Qbeta). In several cases the amount of plaques was diminished or increased depending on the kind of triazine and virus. The investigations demonstrate the triazines to be able to interfere with the formation of plaques by virulent and temperate viruses of procaryotes.

Bacteriophages↗
PubMed1979

Triazine herbicide residues in central European streams.

Triazine herbicide residues were monitored in the rivers Adour, Danube, Garonne, Herault, Loire, Marne, Oise, Rhine, and Rhône from spring 1976 to fall 1977 to determine whether the continued use of the compounds resulted in accumulations of undesirable residues in the streams. Samples were generally collected monthly or bimonthly and analyzed for the parent compounds atrazine, simazine, terbumeton, terbuthylazine, and dealkylated metabolites GS 26571 (2-amino-4-etert-butylamino-6-methoxy-1,3,5-triazine) and G 30033 (2-amino-4-chloro-6-ethylamino-1,3,5-triazine). The compounds were extracted into dichloromethane and quantitated by gas chromatography (GC) with nitrogen-specific detection. Selected results were verified by GC with mass fragmentographic detection. Limit of detection was usually 0.4 mg/m3; 80 percent of all results were below 0.4 mg/m3, 14 percent were 0.4-1 mg/m3, 6 percent were 1-10 mg/m3, and 0.3 percent were higher than 10 mg/m3. Detectable residues were mainly atrazine from the downstream sampling sites. Residues usually peaked during June.

Europe↗
PubMed1977

Mutagenicity of the triazine herbicides atrazine, cyanazine, and simazine in Drosophila melanogaster.

Assays for dominant lethal mutations, sex-linked recessive lethal mutations, and chromosomal breakage, nondisjunction and loss were performed on Drosophila melanogaster males treated by injection or by larval feeding of the herbicides atrazine (2-chloro-4-ethylamino-6-isopropylamino-1,3,5-triazine), cyanazine [2-chloro-4-(1-cyano-1-methylethylamino)-6-ethylamino-1,3,5-triazine], or simazine [2-chloro-4,6-bis-(ethylamino)-1,3,5-triazine]. The three herbicides significantly increased the rate of apparent dominant lethals, but this reduction in egg hatch was probably due to physiologic toxicity to sperm. Atrazine significantly increased X-linked recessive lethals and X or Y loss after treatment by larval feeding. Injection of simazine elevated X-linked lethals, whereas treatment by larval feeding did not. None of these herbicides significantly increased partial loss of the Y chromosome nor sex chromosome nondisjunction. Much larger experiments are needed to determine with confidence the mutagenic potential of these herbicides.

Animals↗
PubMed1978

Synthesis of as-triazines as potential antiviral agents.

Four acenaphtho[1,2-e]-as-triazines and 11 5,6-diaryl-as-triazines, all substituted with an aliphatic or aromatic amino function in the 3-position, were synthesized. Two acenaphthotriazines were active against vesicular stomatitis virus in tissue culture.

Animals↗
PubMed1977

Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.

As part of the search for new antimalarial drugs, a screening program was developed using sensitive and chlorguanide triazine (CGT, cycloguanil) resistant strains of the folate-requiring bacteria, Streptococcus faecium durans, Lactobacillus casei, and Pediococcus cerevisiae. The activities of 40 compounds have been studied against these strains and Escherichia coli. Observations have been made on the points of 50% growth inhibition, the fold increase of resistance shown to each compound by the resistant strains as compared with the parent sensitive strains, and the reversal of growth inhibition by folic acid with S. faecium and L. casei by folinic acid with P. cerevisiae and by p-aminobenzoic acid with E. coli. Comparisons have been made of the activities of the test compounds with those of the standard antimalarial antifoltes, CGT and pyrimethamine (PM), and the antibacterial results have been compared with the activities of the compounds against Plasmodium berghei infections in the mouse and against human malaria infections where data are available. Of the 17 compounds reversed by folates, five had patterns of activity similar to CGT and PM in that they were most active against S. faecium and nine compounds exhibited a different pattern, being highly active against all four test bacteria. This suggests that these latter compounds either have different pharmacokinetic properties or have additional modes of action. The three CGT-resistant organisms responded to antifolates in different ways. S. faecium (R) and P. cerevisiae (R) strains were cross resistant to 4,6-diaminotriazines, 2,4-diaminopyrimidines, 2,4-diaminoquinazolines, and active 2,4-diaminopteridines. L. casei (R) was cross resistant to the triazines but was collaterally sensitive to all the other antifolates. Most of the compounds not reversed by folates were much less inhibitory for the test organisms; they were most active against L. casei. In general, their growth inhibitory concentrations varied less for the four test organisms and the responses of the sensitive and CGTR strains were similar. However, there was some cross resistance to five compounds and some collateral sensitivity to five others. Comparison of the bacteriological data with the activities of the compounds against Plasmodium berghei in the mouse showed little correlation between the two test systems; each appears to provide independent and useful information.

Animals↗
PubMedDate not supplied

Metabolism of 2-(3-chloro-4(4-chlorobenzoyl)-phenyl)-as-triazine-3,5(2H,4H)-dione by the chicken.

The metabolism of the anticoccidial 2-[3-chloro-4-(4-chlorobenzoyl)phenyl]-as-triazine-3,-5(2H,4H)-dione (CP-25,415) was investigated in the chicken. It was shown that the predominant residue present in the chicken was 2-[3-chloro-4-(alpha-hydroxy-4-chlorobenzoyl)phenyl]-as-triazine-3,5(2H,4H)-dione (CP-25,641). A gas-liquid chromatographic assay for the analysis of CP-25,641 in biological fluids and tissues was developed which was rapid, accurate, and reproducible. Results of the analytical method correlated well with radiochemical measurements and were indicative of the total drug-related residues. The half-life of CP-25,641 in tissues was approximately 32 hr except in the kidney, where the half-life was approximately 40 hr due to urine retention by the kidneys. CP-25,641 was excreted without further change.

Adipose Tissue↗
PubMed1979

[Quantitative aspects of the relationship of the antitumor activity and toxicity of diaziridinyl-sym. triazines to their physicochemical properties].

The experiments on rats have shown that there is a linear dependence of the logarithms of reciprocal molar toxic (LD50) and therapeutic (ED50) for sarcoma 45 doses of 6-oxyalkyl-amino-2,4-bis(I-aziridinyl)-sym-triazines and 6-(5-substituted-2,2-dimethyl-1,3-dioxan-5-yl)-amino-2,4-bis(I-aziridinyl)-sym-triazines upon the induction constants of substituents at tertiary carbon, the antitumor activity being more sensitive to the substituent effect compared with the toxicity. The dependence of the logarithms of reciprocal molar therapeutic (ED50 for sarcoma 45 and ED95 for Walker sarcoma) and toxic (LD50 and LD100) doses of the compounds, both synthesized by us and taken from the literature, upon the logarithms of their distribution coefficients in the octanol-water system (IgP) shows a parabolic character with the maximum effect at the extreme point of the parabola. The antitumor activity was more sensitive to a changed IgP than the toxicity.

Animals↗
PubMed1979

The use of sym-triazine trichloride in RNA-protein cross-linking studies with Escherichia coli ribosomal subunits.

The reagent sym-triazine trichloride is used as a bifunctional reagent to generate RNA-protein cross-links within intact ribosomal subunits from E. coli. The reaction takes place in a stepwise manner, involving substitution of one chlorine atom at 12 degrees and pH 8, and substitution of the second at 40 degrees and pH 6. The cross-linked proteins are analysed by two-dimensional electrophoresis, and the existence of a stable cross-linkage is demonstrated by isolating protein-oligonucleotide complexes from 32P-labelled subunits. The proteins cross-linked are S3 and S4 in the 30S subunit, and L2 in the large subunit, together with smaller amounts of other proteins. The reagent should prove useful in topographical studies of the E. coli ribosome as it is a rigid molecule and generates very short cross-links.

Electrophoresis↗
PubMed1976

Hexahydro, 1,3,5, tris (2-hydroxyethyl) triazine, a new bacteriocidal agent as a cause of allergic contact dermatitis.

During the investigation of an outbreak of dermatitis in a medium-sized engineering works, the authors discovered four patients with allergic contact sensitivity to hexahydro,1,3,5, tris (2-hydroxyethyl) triazine, (Grotan), a new bacteriocidal agent used in coolant liquids. The authors failed to find any published report on this subject and would like to draw attention to Grotan as a new potential sensitizer.

Adult↗
PubMed1979

[Carcinogenic effect of the 3-di-(hydroxymethyl-)amino-6-(5-nitro-2-furylethenyl-)1,2,4-triazines in Panfuran-S on mice].

The carcinogenic activity of Panfuran-S containing 3-di-(hydroxymethyl-)amino-6-(5-nitro-2-furylethenyl-)1,2,4-triazine (DHNT) orally administered to mice for 35 weeks was studied. DHNT produced malignant tumors of the forestomach in the highest incidence and also, in decreasing order of frequency, of the duodenum and/or jejunum, esophagus and urinary bladder. Forestomach squamous cell carcinomas were produced dose-dependently in mice receiving more than 350 ppm DHNT and rose to 100% in mice receiving 3,500 ppm. The incidence of duodenal and/or jejunal adenocarcinomas were 8 of 28 mice (29%) receiving 1,750 ppm and 10 of 17 mice (59%) receiving 3,500 ppm. The incidence of esophageal squamous cell carcinoma was 3 of 11 mice (11%) receiving 1,750 ppm and that of urinary bladder transitional cell carcinoma was 2 of 28 mice (7%) receiving 1,750 ppm and 1 of 17 mice (6%) receiving 3,500 ppm DHNT.

Animals↗
PubMed1979

Antiphytoviral activity of 2,4 dioxo hexahydro triazine.

Three treatments with 2,4 dioxo hexahydro triazine (DHT) significantly reduced the concentration of potato virus X (PVX) in systemically infected tobacco plants. In hypersensitive plants DHT caused a reduction in the number of local lesions produced by PVX. In systemic and hypersensitive hosts, treatment with DHT resulted in a more or less marked reduction in the concentration of, and in the number of local lesions caused by, potato virus Y (PVY), potato virus A (PVA), tobacco mosaic virus (TMV), and cucumber mosaic virus (CMV). Three days after treatment with DHT the incorporation of 32P into TMV RNA was significantly reduced, while that into host RNA was less affected.

Antiviral Agents↗