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Pyrazine Derivatives (pyrazine + derivative)
Selected AbstractsNovel Approach to the Synthesis of Perhydropyrazino[1,2-a]pyrazine Derivatives from Amino Alcohols.CHEMINFORM, Issue 18 2006Tatyana V. Lukina Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Oxovanadium(IV) Complexes with Pyrazinecarboxylic Acids:The Coordinating Properties of Ligands with the (Naromatic, COO,) Donor SetEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 13 2006Eugenio Garribba Abstract Complex formation between the VIVO ion and four pyrazine derivatives, 2-pyrazinecarboxylic acid (pzc), 5-methyl-2-pyrazinecarboxylic acid (5-Mepzc), 2,3-pyrazinedicarboxylic acid (3-COOHpzc) and 5-hydroxy-2-pyrazinecarboxylic acid (5-OHpzc), was studied in aqueous solution and in the solid state through the combined application of potentiometric and spectroscopic (EPR and FT-IR) techniques. The results indicate that in acidic and neutral aqueous solution all theligands form mono(chelated), bis(chelated) and dinuclear species of composition VOL, VOL2 and (VO)2L2H,2. Hexacoordinated VOL2 complexes are characterised by a cis/trans isomerism, where cis and trans are the species with a water molecule bound in the cis or trans position with respect to the V=O group. The trans arrangement is favoured over the cis arrangement. Three solid derivatives, [VO(5-Mepzc)2] (1), cis -[VO(pzc)2(H2O)] (2) and cis -[VO(3-COOHpzc)2(H2O)] (3), were isolated and characterised. Based on the experimental results and on the data in the literature, the stability of cis and trans isomers in aqueous solution and in the solid state has been discussed, showing that with ligands of comparable basicity and size of the chelate ring the hydrophilicity favours the cis species and determines the relative amount of the two isomers. The analysis of the magnetic properties of the hydroxo-bridged VIVO dimers suggests that for the (VO)2L2H,2 species the anti -coplanar arrangement is realised. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006) [source] Characterization of volatile compounds and triacylglycerol profiles of nut oils using SPME-GC-MS and MALDI-TOF-MSEUROPEAN JOURNAL OF LIPID SCIENCE AND TECHNOLOGY, Issue 2 2009Stefanie Bail Abstract Several nut oil varieties mainly used as culinary and overall healthy food ingredients were subject of the present study. Headspace solid-phase microextraction combined with gas chromatography-mass spectrometry was employed in order to determine the qualitative composition of volatile compounds. Furthermore, matrix-assisted laser desorption/ionization time-of-flight mass spectrometry was used in order to assess the profiles and relative composition of the prevalent triacylglycerols (TAG) within the oils. The headspace of the majority of oil samples was dominated by high contents of acetic acid (up to 42%) and hexanal (up to 32%). As nut oils are typically gained by cold-pressing from previously roasted nuts, characteristic pyrazine derivatives as well as degradation products of long-chain fatty acids were detected. TAG analysis of these oils revealed a quite homogeneous composition dominated by components of the C52 and C54 group composed mainly of oleic (18:1), linoleic (18:2), stearic (18:0) and palmitic (16:0) acid residues representing together between 65 and 95% of the investigated nut oils. The TAG profiles showed characteristic patterns which can be used as ,fingerprints' of the genuine oils. Nut oils exhibiting quite similar fatty acid composition (e.g. hazelnut, pistachio and beech oil) could be clearly discriminated based on TAG showing significant differences between the oils. [source] First Propargyl Azides Bearing Strong Acceptor Substituents and Their Effective Conversion into Allenyl Azides: Influence of the Electronic Effects of Substituents on the Reactivity of Propargyl Azides,,EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 17 2005Joseph Rodolph Fotsing Abstract We have succeeded in the synthesis of propargyl azides containing 1- or 3-phenylthio functionalities. The selective oxidation of their sulfur atoms to sulfoxides and sulfones allows access to the first propargyl azides bearing acceptor substituents. Interestingly, the prototropic rearrangement of the latter propargyl azides leads to the formation of allenyl azides with relatively high stabilities and with moderate to good yields. Propargyl azides containing phenylthio functionalities react in the presence of nucleophiles to afford the expected N -unsubstituted 1,2,3-triazoles via short-lived allenyl azides. These results are entirely different from those of the corresponding sulfoxides and sulfones, which react under the analogous conditions either to produce the corresponding bis(triazolo)pyrazine derivatives or to yield newly substituted vinyl azides. The latter compounds can successfully be used as starting material providing access to azirines. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005) [source] Studies on the quantitative relationship between the olfactory thresholds of pyrazine derivatives and their molecular structuresFLAVOUR AND FRAGRANCE JOURNAL, Issue 2 2009Feng Luan Abstract Quantitative structure,property relationship (QSPR) investigation was performed for the study of olfactory thresholds of pyrazine derivatives. Descriptors calculated from the molecular structures alone were used to represent the characteristics of the compounds. The six molecular descriptors selected by the best mutilinear regression (BMLR) in CODESSA were used as inputs for support vector machine (SVM) and radial basis function neural networks (RNFNN). The root mean squared errors (RMS) of logarithm of olfactory thresholds (p.p.m.) for the training, predicted and overall datasets were 0.5674, 0.6601 and 0.5860 for BMLR, 0.4720, 0.6861 and 0.5194 for RBFNN, and 0.5242, 0.6466 and 0.5495 for SVM, respectively. The prediction results were in agreement with the experimental values. The QSPR models provide a rapid, simple and valid way to predict the odour threshold of pyrazine derivatives. Copyright © 2009 John Wiley & Sons, Ltd. [source] Aminolevulinic acid-loaded Witepsol microparticles manufactured using a spray congealing procedure: implications for topical photodynamic therapyJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 9 2009Rasil Al-Kassas Abstract Objectives The aim was to enhance aminolevulinic acid (ALA) stability by incorporation into low-melting microparticles prepared using a spray congealing procedure and to evaluate temperature-triggered release, allowing topical bioavailability following melting at skin temperature. Methods ALA-loaded Witepsol microparticles were prepared using a novel spray congealing technique. Entrapment efficiency was compared with conventional emulsion-based methods and modelled drug release profiles determined using a membrane separation technique. Raised receiver medium temperature was used to determine triggered release. Bioavailability and lipid-mediated enhancement of ALA penetration were determined in excised murine skin. Key findings ALA-loaded Witepsol microparticles were spherical, with a mean diameter of 20 ,m. Loading and stability studies demonstrated effective encapsulation, ranging from 91% to 100%, with no evidence of degradation to pyrazine derivatives. ALA release correlated with dissolution medium temperature, triggered at temperatures close to that of skin. Results suggested that molten Witepsol enhanced cutaneous permeation, whereas incorporation of microparticles in a semi-solid vehicle attenuated ALA penetration. Optimal use was direct application under occlusion. Conclusions Spray congealing is superior to the emulsion-based procedures with respect to encapsulation efficiency of ALA in Witepsol matrices, providing temperature-triggered release, enhanced stability and improved penetration of ALA through keratinised skin. These features could improve ALA delivery to superficial lesions as part of photodynamic therapy. [source] | ||||||||||