[Radioprotective action of nitrogenated heterocyclic compound derivatives of imidazole and benzimidazole].
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The synthesis of 9-substituted-pyrido[1,2-a]pyrimidines are described. The new compounds exhibit antiatherosclerotic effects. The 3-ethoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-9-acetic acid (Chinoin-123) has the most favourable effects.
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Glutaconic esters bearing a 2-naphthylamino moiety and a carbethoxy group at the 4-position underwent thermal decomposition to give 1-carbethoxy-3H-benz[e]indole derivatives. Alkaline hydrolysis of 1-carbethoxy-3H-benz[e]indoles gave the corresponding 3H-benz[e]indoles by loss of the carboxylic group. By this method were synthesized the known 3H-benz[e5indole and the 7-methoxy-3H-benz[e]indole. Glutaconic esters used in this procedure were prepared by condensation of ethyl propiolate with the appropriate 2-naphthylaminomalonate ethyl ester in the presence of a catalytic amount of sodium ethylate.
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In recent years there has been increasing interest on studies concerning indoor air quality and focusing on risk factors for exposed subjects. Particularly, airborne chemicals, whose adverse effects are well known, have been identified and determined in means of transport as in other indoor places. As concerns chemical air concentrations in submarines, only a limited number of studies have been published. This paper reports measured concentration data for organic compounds (total volatile organic compounds, substances with a chemical bond S-O, nitrogen compounds, carbon monoxide, carbon dioxide, and different organic solvents) in the air sampled during an 8-h period in an Italian Military submarine, under routine operations. We observed that a periodicalfresh-air intake operation (snorkel) might cause temporary increase of contaminants levels in indoor air. Moreover, we could find that pollutants sometimes reach notable peak concentrations being potentially able to induce adverse health effects in crewmembers. Our data highlight the need to promote further investigations.
Capillary gas chromatography with nitrogen-specific detection allows rapid screening of numerous drugs of toxicological interest. However, for accurate identification of individual peaks, the system must be well calibrated, e.g., through the use of retention indices (RI). To overcome problems associated with the use of RI's based on homologous series determined with nitrogen-specific detectors, we have developed an RI reference system based on molecular masses and retention times of nitrogen-containing compounds. The standards chosen are easily available in highly purified form and can be detected by the unmodified nitrogen-specific detector. By using temperature programming, we can obtain a linear relationship between the molecular masses of standards and their retention times. Used in conjunction with microcomputer data handling, this screening system is rugged and reliable, operating 22 h per day. In the past two years, we have screened greater than 3000 samples (blood, serum, urine, gastric lavage) without major problems.
Isolated human neutrophilic leukocytes were stimulated to produce hydrogen peroxide (H2O2) and to secrete cytoplasmic granule components including myeloperoxidase into the medium. Myeloperoxidase catalyzed the oxidation of chloride (Cl-) by H2O2 to yield hypochlorous acid (HOCl), which reacted with endogenous nitrogen compounds to yield derivatives containing nitrogen-chlorine (N-Cl) bonds. Compounds available for reaction with HOCl were ammonia (NH+4), taurine, alpha-amino acids, and granule proteins and peptides that were released into the medium. A portion of the N-Cl derivatives formed under these conditions accumulated in the extracellular medium. These long lived oxidizing agents were characterized as hydrophilic, low molecular weight, mono-N-chloramine (RNHCl) derivatives based on their absorption spectrum, ability to oxidize 5-thio-2-nitrobenzoic acid and to chlorinate ammonia (NH+4), and behavior upon ultrafiltration, gel chromatography, and extraction with organic solvents. The RNHCl derivatives were of low toxicity, but reacted with NH+4 to yield the lipophilic oxidizing agent monochloramine (NH2Cl). Therefore, the addition of NH+4 conferred bactericidal, cytotoxic, and cytolytic activities on the RNHCl derivatives. The results indicate that taurine and other neutrophil amines protect neutrophils and other cells against oxidative attack by acting as a trap for HOCl and by competing with endogenous NH+4 for reaction with HOCl. However, the RNHCl derivatives act as a reserve of oxidizing equivalents that is converted to a toxic form when an increase in NH+4 concentration favors formation of NH2Cl.
The effects of nitrate, ammonium, and urea as nitrogen sources on the heterotrophic growth of Chlorella protothecoides were investigated using flask cultures. No appreciable inhibitory effect on the algal growth was observed over a nitrogen concentration range of 0.85-1.7 g l(-)(1). In contrast, differences in specific growth rate and biomass production were found among the cultures with the various nitrogen compounds. The influence of different nitrogen sources at a concentration equivalent to 1.7 g l(-)(1) nitrogen on the heterotrophic production of biomass and lutein by C. protothecoides was investigated using the culture medium containing 40 g l(-)(1) glucose as the sole carbon and energy source in fermentors. The maximum biomass concentrations in the three cultures with nitrate, ammonium, and urea were 18.4, 18.9, and 19.6 g l(-)(1) dry cells, respectively. The maximum lutein yields in these cultures were between 68.42 and 83.81 mg l(-)(1). The highest yields of both biomass and lutein were achieved in the culture with urea. It was therefore concluded that urea was the best nitrogen source for the production of biomass and lutein. Based on the experimental results, a group of kinetic models describing cell growth, lutein production, and glucose and nitrogen consumption were proposed and a satisfactory fit was found between the experimental results and predicted values. Dynamic analysis of models demonstrated that enhancing initial nitrogen concentration in fermentor cultures, which correspondingly enhances cell growth and lutein formation, may shorten the fermentation cycle by 25-46%.
The effect of dietary pectin on apparent ileal and fecal digestibilities of protein and amino acids and on pancreatic secretions was studied in two experiments with growing pigs (initial weight 70 kg). Four barrows were fitted with simple T-cannulas for collection of ileal digesta; another four barrows were fitted with permanent re-entrant cannulas for collection, sampling and subsequent return of pancreatic juice. Dietary pectin included at a level of 7.5 g/100 g in a cornstarch-based diet significantly depressed apparent ileal and fecal protein and amino acid digestibilities. This depression in the small intestine could be attributed to both an increase in endogenous protein secretions and a decrease in the efficiency of digestion. In the large intestine, pectin was used by intestinal microbes as the principal energy source to catabolize nitrogenous compounds and to stimulate bacterial nitrogen assimilation, thus altering the amino acid profile of protein voided in feces. The inclusion of pectin did not affect the flow of pancreatic juice or the total secretion of protein, lipase, trypsin and chymotrypsin. However, there was a significantly lower secretion of alpha-amylase, which was a direct result of the replacement of starch by pectin. The results demonstrate that pectin may have a detrimental effect on the processes of protein digestion and absorption but does not affect the secretion of pancreatic proteolytic enzymes in pigs.
Ammonia oxidizing bacteria extract energy for growth from the oxidation of ammonia to nitrite. Ammonia monooxygenase, which initiates ammonia oxidation, remains enigmatic given the lack of purified preparations. Genetic and biochemical studies support a model for the enzyme consisting of three subunits and metal centers of copper and iron. Knowledge of hydroxylamine oxidoreductase, which oxidizes hydroxylamine formed by ammonia monooxygenase to nitrite, is informed by a crystal structure and detailed spectroscopic and catalytic studies. Other inorganic nitrogen compounds, including NO, N2O, NO2, and N2 can be consumed and/or produced by ammonia-oxidizing bacteria. NO and N2O can be produced as byproducts of hydroxylamine oxidation or through nitrite reduction. NO2 can serve as an alternative oxidant in place of O2 in some ammonia-oxidizing strains. Our knowledge of the diversity of inorganic N metabolism by ammonia-oxidizing bacteria continues to grow. Nonetheless, many questions remain regarding the enzymes and genes involved in these processes and the role of these pathways in ammonia oxidizers.