Synthesis of Some New Folic Acid-Based Heterocycles of Anticipated Biological Activity

To date, no fused heterocycles have been formed on folic acid molecules; for this reason, and others, our target is to synthesize new derivatives of folic acid as isolated or fused systems. Folic acid 1 reacted with ethyl pyruvate, triethyl orthoformate, ethyl chloroformate, thioformic acid hydrazide, and aldehydes to give new derivatives of folic acid 2–6a,b. Moreover, It reacted with benzylidene malononitrile, acetylacetone, ninhydrin, ethyl acetoacetate, ethyl cyanoacetate, and ethyl chloroacetate to give the pteridine fused systems 10–15, respectively. Ethoxycarbonylamino derivate 5 reacted with some nucleophiles containing the NH₂ group, such as aminoguanidinium hydrocarbonate, hydrazine hydrate, glycine, thioformic acid hydrazide, and sulfa drugs in different conditions to give the urea derivatives 16–20a,b. Compound 4 reacted with the same nucleophiles to give the methylidene amino derivatives 21–24a,b. The fused compound 10 reacted with thioglycolic acid carbon disulfide, malononitrile, and formamide to give the four cyclic fused systems 25–30, respectively. The biological activity of some synthesized showed moderate effect against bacteria, but no effect shown towards fungi.     

Correlation between floppy to rigid transitions and non-Arrhenius conductivity in glasses

Non-Arrhenius behavior is observed for a number of virgin potassium silicate glasses (1-x)SiO2-xK2O with a potassium oxide concentration larger than a certain value x = x(c). Recovering of Arrhenius behavior is provided by the annealing that enhances densification. These various results are the manifestation of the floppy or rigid nature of the network. Compositional effects and saturation with temperature can be analyzed with a combination of constraint theory and a point defect model. They underscore the key role played by network rigidity for the understanding of conduction and saturation effects in glassy electrolytes.     

Studies on the Reduction of the Nitro Group in 4-Nitroindazoles by Anhydrous SnCl2 in Different Alcohols

The bakers' yeast reduction of a number of alkyl levulinates occurs in good to moderate yields to give the corresponding (S) alcohols in > 98% ee. The (S) alcohol la has been converted to synthetically useful (S)- or (R)-4- methylbutyro-lactone and (S)-(+)-l,4-pentanediol in good yields.     

'In situ' Edman degradation of protein(s) blotted to immobilon membranes suitable for unblocking reversible chemical modification and elimination of coomassie blue in sodium dodecyl sulfate-polyacrylamide gel electrophoresis

Conditions for unblocking reversible chemical modifications such as maleylation or citraconylation 'in situ' at the N-terminus of proteins after transfer of proteins to immobilon membranes from SDS-PAGE are described. Demaleylation or decitraconylation occurred at 55 degrees C in 70% formic acid (pH 1.50) during 60 min. During the unblocking reaction, Coomassie blue dye was completely removed, resulting in superior high performance liquid chromatographic separation of phenylthiohydantoin-amino acid (PTH-AA) after Edman degradation (automatic gas phase sequencer). The protein fixed on the matrix after demaleylation and removal of Coomassie blue was not degraded. The possible cleavage at the aspartyl-prolyl peptide bonds was considered, but no side reaction was observed. Furthermore, the incubation time in 70% formic acid at 55 degrees C could be reduced to 10 min in the absence of maleylation of the starting material, and this was suitable for the removal of Coomassie blue and the quantification of phenylthiolhydantoin-amino acids (PTH-AAs) by HPLC. The yield from the starting protein through SDS-PAGE, blotting, and Edman degradation to quantitative analysis of PTH-aminoacid(s) by HPLC was established.     

A coupled blade element momentum – Computational fluid dynamics model for evaluating tidal stream turbine performance

A modelling approach based on blade element momentum theory is developed for the prediction of tidal stream turbine performance in the ocean environment. Through the coupling of the blade element momentum method with computational fluid dynamics, the influence of upstream hydrodynamics on rotor performance is accounted for. Incoming flow onto the rotor can vary in speed and direction compared to free-stream conditions due to the presence of obstructions to the flow in the upstream, due to other devices for example, or due to the complexity of natural bathymetries. The relative simplicity of the model leads to short run times and a lower demand on computational resources making it a useful tool for considering more complex engineering problems consisting of multiple tidal stream turbines. Results from the model compare well against both measured data from flume experiments and results obtained using the classical blade element momentum model. A discussion considering the advantages and disadvantages of these different approaches is included.     

Fast-ion conduction and flexibility of glassy networks

We observe two thresholds in the variations of electrical conductivity of dry (AgI)_{x}(AgPO3)_{1-x} solid electrolyte glasses, when the AgI additive concentration x increases to 9.5% and to 37.8%. Raman scattering complemented by calorimetric measurements confirms that these thresholds are signatures of the rigidity phase transitions at x=9.5% from a stressed rigid to an isostatically (stress-free) rigid phase, and at x=37.8% from isostatically rigid to a flexible phase. In the flexible phase, the electrical conductivity seems to increase as a power of x. This is in good agreement with the theoretical prediction based on 3D percolation.     

Discommensuration observed through 133Cs N.M.R. in stage II cesium-graphite intercalation compounds

An apparent transition is observed at 120 K in stage II Cs-GIC's through ¹³³Cs NMR: the line splits into a small number of individual components which all shift abruptly downfield with further increasing T. Such a shift is due to an increase of the s-character of the conduction electron wave-functions at Fermi energy. The results are interpreted in terms of a discommensuration between the graphitic and the metallic lattices.