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At least 721 records · Page 40Linked to original sources
PubMed1993

Synthesis of some new thioethers of 1,2,4-triazine-3-hydrazones and assays for their anticancer and anti human immune virus activities.

A number of various thioethers derived from 3-hydrazone-5,6-diphenyl-1,2,4-triazines have been synthesized and evaluated for anticancer and anti HIV activities. The structures are supported by elemental analysis, IR, UV and 1H-NMR spectral data. Most of the tested compounds displayed a significant activity against Leukemia/Lymphoma, CNS, Ovarian and Small cell lung cancer.

Antineoplastic Agents↗
PubMed1993

Synthesis of some new 4,6-disubstituted-1,2,4-triazin-3,5(2H) diones and related compounds of potential antifungal activity.

The synthesis of 4-substituted amino-6-styryl/alkyl/aryl-1,2,4-triazin- 3,5(2H)diones (4a-d and 15) involving the cyclocondensation of N4-arylaminosemicarbazides(3a-d and 13) with some alpha-ketoacids is described. The behaviour of these triazinones towards amine, hydrazine, isothiocyanate, aromatic aldehyde and gl. acetic acid have been investigated. Structure elucidation of the new compounds has been carried out with the help of elemental analysis, IR, UV and 1H-NMR spectra. The antifungal activity of the prepared compounds has been assayed both in vitro and in vivo against some phytopathogenic fungi associated with wheat grains, were the compound 3b showed a high protection of the grains of wheat against the fungal infection.

Fungi↗
PubMed1996

1H-pyrazolo[4,3-d]pyrimidine-7(6H)-one and 5H-pyrazolo[4,3-d] 1,2,3-triazin-4(3H)-one derivatives. Synthesis and in vitro biological activity at adenosine A1 and A2a receptors.

The affinity of newly synthesized 1H-pyrazolo[4,3-d] pyrimidine-7 (6H)- one (5a-f) and 5H-pyrazolo[4,3-d]1,2,3,-triazin-4(3H)-one (6a-i) derivatives for A1 and A2a adenosine receptors was investigated in rat cerebral membranes. The compounds showed affinities in the micromolar range for both adenosine A1 and A2a receptors. In particular 5d was the most interesting compound and showed some degree of selectivity for the A1 receptor (Ki values being 2 mumol/l; A1/A2a ratio < 0.021). The present study provides useful information for a better understanding of the structure-activity relationships of antagonists at adenosine receptors.

Adenosine↗
PubMed1996

Anti-HIV activity of some non-nucleoside s-triazine derivatives (Part-IV).

2-(4-Methoxy/2-methyl phenyl)-4-phenyl acetyl hydrazino-6-isonicotinyl hydrazino-s-triazines (1a-b) have been synthesized and tested for their anti-HIV activity against susceptible human host cell (CEM cell line), over a wide range of concentrations. The synthesized compounds have been found moderately active as compared to AZT.

Antiviral Agents↗
PubMed1995

125I-4-(2-[7-amino-2-[2-furyl][1,2,4]triazolo[2,3-a][1,3,5] triazin-5-yl-amino]ethyl)phenol, a high affinity antagonist radioligand selective for the A2a adenosine receptor.

The A2a adenosine receptor (AR) mediates several important physiological effects of adenosine, including vasodilation and inhibition of platelet aggregation. Until recently, no antagonist radioligand of sufficient selectivity or affinity was available. We describe the synthesis and characterization by radioligand binding of 125I-4-(2-[7-amino-2-{2-furyl}-{1,2,4}triazolo{2,3-a}- {1,3,5}triazin-5-yl-amino]ethyl)phenol (125I-ZM241385) in membranes from two cell types that express A2a ARs. Membranes from Chinese hamster ovary (CHO) cells expressing a recombinant canine A2a AR bound 125I-ZM241385 with high affinity, and agonist competition experiments with 2-(p-carboxyethyl)-phenylamino-5'-N-carboxamidoadenosine, 5'-N-ethylcarboxamidoadenosine, and (-)-N6[(R)-phenylisopropyl]adenosine revealed a potency order characteristic of an A2a AR binding site. Membranes from bovine striatum, which contain a native A2a AR, also bound 125I-ZM214385 with similarly high affinity and also displayed a pharmacological profile for displacement of radioligand binding that was consistent with that of an A2a AR. Also, under conditions in which 125I-ZM241385 bound with high affinity to a recombinant rat A2a AR expressed in CHO cells, no specific binding was detectable in membranes from CHO cells expressing functional rat A1, A2b, or A3 ARs, indicating that over the range of concentrations used in radioligand binding assays, 125I-ZM214385 is a highly selective antagonist radioligand for study of A2a ARs within a given species.

Animals↗
PubMed1997

Synthesis and biological activity studies of 1,3,4-thiadiazolo[2,3-c]-as-triazines.

Several new 1,3,4-thiadiazolo[2,3-c]-as-triazines were synthesized by the reaction of 6-substituted-4-amino-3-mercapto-1,3,4-triazon-5 (4H)-ones with appropriate aromatic and heterocyclic carboxylic acids in the presence of phosphorus oxychloride. The structures of the newly synthesized compounds were established on the basis of analytical, IR, NMR and mass spectral data. Some selected compounds from this series were subjected to both antimicrobial and pharmacological studies.

Animals↗
PubMedDate not supplied

Bicyclic [b]-heteroannelated pyridazine derivatives. Part 5. Synthesis of some triazolo[4,3-b]pyridazine and pyridazino[6,1-c]triazine derivatives as potential benzodiazepine receptor ligands.

4-Substituted-tetrahydropyridazine-3,6-dione 3-hydrazones [I] reacted with strong carboxylic acids and some acyl chlorides to give the N-acylation products and/or triazolo[4,3-b]pyridazine derivatives. Derivatives of this bicyclic structure were obtained also in reactions of I with triethyl orthoformate and orthoacetate. In the reaction with phosgene, triazolo[4,3-b]pyridazine-3,6-dione, and with oxalyl chloride pyridazino[6,1-c]triazine-3,4,7-trione derivatives were obtained.

Animals↗
PubMed1998

Studies on arylmethyltriazinone derivatives-Part II. Synthesis and antifungal properties of 2-aminomethyl-4-(arylidene)amino-6-arylmethyl- 3-mercapto-1,2,4-triazin-5(4H)-ones.

The preparation of twenty new 2-aminomethyl-4-(arylidene)amino- 6-arylmethyl-3-mercapto-1,2,4-triazin-5(4H)-ones(4) is described. The structural elucidation of all the compounds is carried out on the basis of analytical and spectral data. The newly synthesized compounds are evaluated for their antifungal activity against Candida albicans and Paecileomyces variotti.

Antifungal Agents↗
PubMed1998

A chemical modification of myeloperoxidase and lactoperoxidase with 2-(O-methoxypolyethylene glycol)-4, 6-dichloro-s-triazine (activated PEG1).

The modification of myeloperoxidase and lactoperoxidase with 2-(O-methoxypolethylene glycol)-4, 6-dichloro-s-triazine, an activated polyethylene glycol (PEG1), was investigated. The modification caused a shift of the Soret band in the light absorption spectrum, from 430 nm to 418 nm in the case of myeloperoxidase (native ferric form), and from 412 nm to 406 nm in the case of lactoperoxidase (native ferric form). PEG1-modified myeloperoxidase and PEG1-modified lactoperoxidase both failed to bind with antiserum to the respective native enzyme, but both retained respectively 4.5 +/- 0.3 per cent (mean +/- SE, n = 5) and 0.6 +/- 0.2 per cent (mean +/- SE, n = 5) of the activities of peroxidation of the hydrogen donor o-methoxyphenol in comparison with the native enzyme, and 1.5 +/- 0.2 per cent (mean +/- SE, n = 5) and 1.2 +/- 0.2 per cent (mean +/- SE, n = 5) of the activities of destruction of fuchsin basic in the presence of hydrogen peroxide and a halide, bromide. The pH dependencies of the peroxidating activities were almost the same as those of the corresponding native enzymes, but both the optimal pHs of the reactions involving the destruction of fuchsin basic were shifted by approximately 1.0 pH unit toward neutral pH compared with the respective native enzymes.

Animals↗
PubMed2004

Structure/activity investigations of 5-substituted 3-methylisoxazole[5, 4-d]1, 2, 3-triazin-4-one derivatives.

The series of 5-substituted 3-methylisoxazole[5, 4-d]1, 2, 3-triazin-4-one derivatives was obtained by diazotization of 5-amino-3-methylisoxazol-4-carboxylic acid hydrazide. The immunological activity of these compounds was investigated experimentally in several in vitro and in vivo assays in mice and human models. In the next step, quantum-chemical investigations were performed using density functional theory with the B3LYP hybrid exchange-correlation energy functional and 6-31G(d, p) basis set. The Polarizable Continuum (SCRF/PCM) solvent model was also taken into account in order to show solvent influence on electron density and electrostatic potential around the exemplary molecules. Correlations between molecular structure and biological properties were found using a stepwise selection of scales for the multiple linear regression (MLR).

Animals↗
PubMed2007

Rapid on-plate and one-pot derivatization of carbonyl compounds for enhanced detection by reactive matrix LDI-TOF MS using the tailor-made reactive matrix, 4-dimethylamino-6-(4-methoxy-1-naphthyl)-1,3,5-triazine-2-hydrazine (DMNTH).

In this study, a very sensitive and economical high-throughput methodology has been developed for the analysis of small carbonyl compounds using rapid derivatization with 4-dimethylamino-6-(4-methoxy-1-naphthyl)-1,3,5-triazine-2-hydrazine (DMNTH), a derivatizing agent developed by the Karst group at the University of Münster. DMNTH is highly ionizable by the UV laser and reacts selectively and rapidly with carbonyl moieties. The resulting hydrazone is easily detectable by laser desorption ionization time of flight mass spectrometry (LDI-TOF MS), eliminating the need for the matrix assisted variant (MALDI) and the associated issue of matrix optimization, which greatly simplifies the analysis. It has been demonstrated that a range of carbonyl compounds can be conveniently analyzed by this reactive matrix LDI-TOF MS (RM-LDI-TOF MS) procedure and that furfural DMNThydrazone (prior labeled and labeled in situ) can be used as an internal standard for semiquantitative analysis. Amounts as low as 0.5 ng ml(-1) of 4-methoxybenzaldehyde have been detected using a one-pot derivatization methodology. Rapid on-plate derivatization was also found to be a simple approach for fast and reliable screening of various analytes, although with slightly higher detection limits. To test its applicability in complex matrices, analysis of furfural spiked in beer has been demonstrated. This RM-LDI-TOF MS method shows considerable promise for the analysis of carbonyl compounds in water, particularly for disinfection by-products that result from reaction of natural organic matter with oxidative disinfectants.

Journal Article↗
PubMed2002

Supramolecular self-assembly of nanotubes and supercoils from long-chain derivatives of pyrimindinetrione and triazine.

The self-assembly of two complementary components, 5-(4-N-methyl-N-dodecylaminobenzylidene)-2,4,6-(1H,3H)-pyrimidi-netrione (1) and 4-amino-2,6-didodecylamino-1,3,5-triazine (2) was found to result in the formation of a hollow supramolecular nanotube with about 6 nm in diameter and hundreds of nanometers in length as observed directly by transmission electron microscope (TEM). X-ray diffraction patterns indicate that a periodical layered structure with a d spacing of 0.49 nm in the nanotube exists. If staining treatment were employed in TEM observations, the self-assembly was found to show a supercoil structure about 300 nm in diameter.

Journal Article↗
PubMed1998

Structure and High-Resolution IR Spectroscopy of 1,2,4-Triazine Vapor.

The high-resolution infrared bands centered at 769 and 1043 cm-1 for 1,2,4-triazine C3H3N3 have been analyzed, using the full asymmetric rotor Hamilton of Watson in A-reduced form using IIIr-representation. All the ground state rotation constants and three of the quartic centrifugal distortion constants could be determined with high precision from a simultaneous analysis of the two bands. The standard deviation of fit was 0.00077 cm-1. The upper state constants for the two bands have been determined with similar precision. The ground state rotational constants obtained from the present analysis are very similar to those predicted from the ab initio study of the equilibrium structure. This strongly suggests that the similarity in several of the ring bond lengths, predicted in the latter, is indeed real. Copyright 1998 Academic Press.

Journal Article↗
PubMed1996

Decomposition Products of s-Triazine Herbicides by Electron-Transfer in Acidic Aqueous Media

The reduction of atrazine and terbutylazine was preceded by protonation equilibrium. Three protonation sites of the s-triazine molecule determined the structure of the final reduction product. Protonation was investigated by the change of UV-Vis spectra. Two slightly different pKs corresponding to protonation on N5 and N1 heteroatoms were evaluated. The principal reduction pathway involved the cleavage of a chlorine atom. A small quantity of desethylatrazine was detected in the most acidic media.

Journal Article↗
PubMed1996

Trace analysis of triazines and organophosphorus pesticides in water.

A method for the determination of trace levels of triazines and organophosphorus pesticides in water is presented. The extraction method is based on a solid-phase extraction on C-18 bound silica SPE cartridges. A precolumn filled with Merck C-18 bound silica and home-made C-18 bound silica have been tested at a flow-rate of 3 ml/min with comparable preconcentration yields. A SIM-MS method using a (15)N labelled internal standard has been developed for the organophosphorus pesticides. Detection limits lower than 1 microg/L have been obtained. Separations have been carried out on a conventional GC column OV 17 (1 m) and a capillary column OV 17 (25 m) with a temperature program from 150 degrees C (2 min) to 300 degrees C (rate of 6 degrees C/min).

Journal Article↗
PubMed1996

Adsorptive stripping voltammetric analysis of 2,4,6-tri(2'pyridyl)-1,3,5-triazine at a mercury electrode.

The redox behaviour of adsorbed species of 2,4,6-tri(2'-pyridyl)-1,3-5-triazine (TPTZ) at the surface of a mercury electrode was examined using cycling voltammetry. Based on the adsorption and accumulation of TPTZ at the charged mercury surface cathodic adsorptive stripping voltammetry (CSV) is applied for the trace determination of TPTZ using a differential pulse (DP) technique. Experimental and operational parameters for the quantitative analysis of TPTZ are optimized and the detection limit was found to be 3x10(-9) mol/l. The effect of some interferences, e.g. organic compounds, cations and anions, are investigated.

Journal Article↗
PubMed2006

In ovo exposure to a triazine herbicide: effects of atrazine on circulating reproductive hormones and gonadal histology in young Japanese quail.

The triazine herbicide, atrazine, has come under scrutiny for its reported feminizing effects in amphibians. To date, there is little information concerning the effects of atrazine on reproduction in avian species. The current study examined the putative reproductive toxicity of atrazine after exposure in ovo. Atrazine at 504, 246, and 123 microg/kg was administered to Japanese quail eggs before incubation. The eggs were hatched and the birds raised to 14 days of age. Indices of hatchability, sex ratios, and growth were determined. Furthermore, circulating concentrations of reproductive hormones (estradiol, progesterone, and testosterone) and gonadal histology were examined. Atrazine at 504 microg/kg decreased 14-day hatchling weight by 13.1% versus controls. However, no detrimental effects on hatchability or sex ratios were observed. In female birds, atrazine at 504 microg/kg decreased ovarian weights and circulating concentrations of progesterone to 48.3% and 73.3%, respectively, versus control. However, concentrations of estradiol and testosterone did not differ from controls. In male quail, at all doses tested, atrazine had no effect on gonadal weights or circulating concentrations of estradiol, testosterone, or progesterone. Moreover, no incidences of left ovotestis formation were observed. In contrast, 10 ng/kg ethinylestradiol (a positive control) induced the formation of a left ovotestis in four of eight birds analyzed. The current results may suggest that exposure to atrazine in ovo at concentrations above ecologic relevance exerts effects on the reproductive system of young Japanese quail. However, no evidence is presented that atrazine induces feminization of the testis in male quail.

Animals↗