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PubMed1986

Gas chromatographic assay for the new antitumor agent pyrazine-2-diazohydroxide (diazohydroxide) and its stability in buffer, blood and plasma.

Diazohydroxide is a new antitumor agent being considered for clinical trial. A sensitive and specific assay for diazohydroxide in physiological media, plasma and blood has been developed based on conversion of diazohydroxide to 2-chloropyrazine in the presence of strong hydrochloric acid. The 2-chloropyrazine is extracted into the ethyl acetate and separated by capillary gas chromatography with nitrogen-phosphorus detection. Using 0.2 ml plasma the assay was linear up to 100 micrograms/ml diazohydroxide and had a lower limit of detectability for diazohydroxide of 50 ng/ml. The coefficient of variation of the assay at 1 micrograms/ml was 6.7%. Breakdown of diazohydroxide was rapid under mild acid conditions but slower under alkaline conditions,. The half-life of diazohydroxide in 0.1 M sodium phosphate buffer, pH 6.0, at room temperature was 5 min and at pH 8.0, 480 min. Breakdown of diazohydroxide in plasma was biphasic. In fresh mouse plasma diazohydroxide had a terminal half-life at 37 degrees C of 72 min while in fresh human plasma the terminal half-life was 23 min and in fresh blood 21 min. Diazohydroxide accumulated in red blood cells at 37 degrees C to a concentration 68% above the concentration in plasma. Diazohydroxide was 49% bound to human plasma proteins at room temperature.

Animals↗
PubMed2003

Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist.

Based on a computational model for 5-HT(1A)R-ligand interaction and QSAR studies, we have designed and synthesized a new series of arylpiperazines 2-8 which exhibit high 5-HT(1A)R affinity and selectivity over alpha(1)-adrenergic receptors. Among them, compound CSP-2503 (4) has been pharmacologically characterized as a 5-HT(1A)R agonist at somatodendritic and postsynaptic sites, endowed with anxiolytic properties.

Amino Acid Sequence↗
PubMed2000

8-Methylureido-10-amino-10-methyl-imidazo[1,2-a]indeno[1,2-e] pyrazine-4-ones: highly in vivo potent and selective AMPA receptor antagonists.

Water soluble 8-methylureido-10-amino-10-methyl-imidazo[1,2-a]indeno[1,2-e]pyraz ine-4-one 4 represents a novel class of highly potent and selective AMPA receptors antagonists with in vivo activity. The dextrorotatory isomer (+)-4 was found to display the highest affinity with an IC50 of 10 nM. It also exhibited very good anticonvulsant effects after i.p., s.c. and i.v. administration in mice subjected to electrical convulsions (MES) and i.p. in audiogenic seizure-e in DBA/2 mice (ED50's < or = 10 mg/kg).

Animals↗
PubMed2005

Mechanism of formation of redox-active hydroxylated benzenes and pyrazine in 13C-labeled glycine/D-glucose model systems.

To extend the analytical capabilities of the pyrolysis-gas chromatograph-mass spectrometry system that has been successfully utilized in the past as an integrated reaction, separation, and identification system to study label incorporation patterns in Maillard reaction products, a novel methodology was developed to analyze the composition of nonvolatile residues of the initial reaction products. This was achieved through a postpyrolytic in-situ derivatization technique using trimethylsilyldiethylamine. Application of this technique to the investigation of the nonvolatile products formed during pyrolysis of glucose alone and in the presence of glycine has indicated the formation of several redox-active hydroxylated benzene derivatives such as 1,2,3-trihydroxybenzene (pyrogallol), 1,4-dihydroxybenzene (hydroquinone), 1,2-dihydroxybenzene (catechol), and 2,5-dihydroxypyrazine. Labeling studies have indicated that the intact glucose carbon backbone was involved in the construction of the benzene ring of the hydroxylated benzene derivatives and that dimerization of glycine alone can lead to the formation of 2,5-dihydroxypyrazine.

Benzene↗
PubMed2000

Synthesis of phenoxyphenyl pyridine and pyrazine carboxamides. Activity against Cydia pomonella (L.) eggs.

Several N-(4-phenoxyphenyl)pyridinecarboxamides and N-(4-phenoxyphenyl)pyrazinecarboxamides were synthesized from commercially available material, and their ovicidal activities against Cydia pomonella (L.) were tested. Some of the tested products showed a moderate activity when <24-h-old eggs were sprayed using a Potter tower. A significant increase in the length of the development period of the eggs was also observed in many cases. A clear correlation between both effects was noticed: the products that produced higher mortality also produced higher increase of the length of the development. These results seem to confirm our hypothesis that these compounds could be defined as a juvenile hormone analogues.

Animals↗