A concise synthesis of tetrahydroisoquinoline-1-carboxylic acids using a Petasis reaction and Pomeranz–Fritsch–Bobbitt cyclization sequence

A sequence of two reactions: the Petasis reaction, in which an aminoacetaldehyde acetal was used as the amine component, followed by Pomeranz–Fritsch–Bobbitt cyclization, has been shown to be a convenient and simple method for the synthesis of tetrahydroisoquinoline-1-carboxylic acids. Using this method several acids have been prepared in good to excellent yields and characterized as hydrochloride salts.     

Analysis of mechanisms with flexible beam-like links,rotary joints and assembly errors

The paper presents a method of modelling dynamics of mechanisms in which assembly errors can occur. One of the features of the method is that such errors can be included when the kinematics of the mechanism is modelled. A closed kinematic chain consisting of flexible and rigid links with one joint displaced and turned is discussed. Use of joint coordinates together with the rigid finite element method for discretisation of flexible links has allowed us to considerably decrease the size of the problem. Numerical simulations are carried out in order to analyse the influence of inaccurate assembly on the load on joints of a four-bar linkage.     

Synthesis of O-[4,6-Di-O-Acetyl-4-O-(2,3,4,6-Tetra-O-Acetyl-β-D-Galactopyranosyl)-2-Deoxy-2-Hydroxyimino-D-Arabino-Hexopyranosyl]-N-Benzyloxycarbonyl-L-Serine Methyl Esters And Their Transformations

ABSTRACT

3,6-Di-O-acetyl-4-O-(2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl)-2-deoxy-2-hydroxyimino-α- and -β-D-arabino-hexopyranosides of N-benzyloxycarbonyl-L-serine methyl ester as well as of ethanol have been synthesised from D-lactal hexaacetate via nitrosyl chloride, followed by condensation with L-serine derivatives and ethanol, respectively. The compounds of L-serine thus obtained were modified at C-2 and C-3 to afford L-serine derivatives attached to disaccharides containing terminal α-D-gluco-, 2-acetamido-α-D-gluco-, β-D-manno, 2-acetamido-β-D-manno-pyranosyl, 3-azido-2-hydroxyimino-α-D-arabino-, and α-D-ribo-hexopyranosyl residues.     

Crystal Structure and Solid State 13C Nmr Analysis of Methyl 3,4,6-Tri-O-Acetyl-2-Deoxy-2-(3-Phenylureido)-β-D-Glucopyranoside

ABSTRACT

The X-ray diffraction analysis of methyl 3,4,6-tri-O-acetyl-2-deoxy-(3-phenylureido)-β-D-glucopyranoside was performed and showed that the molecules are associated by two NHz.O=C hydrogen bonds. One molecule with disorder of an acetyl group at C-4 was found in the asymmetric crystal unit. The signals in ¹³C CPMAS NMR spectrum are duplicated indicating that local symmetry is lower than those of the crystal.     

Polycationic Pillar[5]arene Derivatives: Interaction with DNA and Biological Applications

Dendritic pillar[5]arene derivatives have been efficiently prepared by grafting dendrons with peripheral Boc‐protected amine subunits onto a preconstructed pillar[5]arene scaffold. Upon cleavage of the Boc‐protected groups, water‐soluble pillar[5]arene derivatives with 20 ( 13 ) and 40 ( 14 ) peripheral ammonium groups have been obtained. The capability of these compounds to form stable nanoparticles with plasmid DNA has been demonstrated by gel electrophoresis, transmission electron microscopy (TEM), and dynamic light scattering (DLS) investigations. Transfection efficiencies of the self‐assembled 13 /pCMV‐Luc and 14 /pCMV‐Luc polyplexes have been evaluated in vitro with HeLa cells. The transfection efficiencies found for both compounds are good, and pillar[5]arenes 13 and 14 show very low toxicity if any.     

New Hybrid Polyurea-Polyurethane Elastomers with Antistatic Properties and an Influence of Various Additives on Their Physicochemical Properties

Polyurea is a synthetic high-strength elastomeric material that can be sprayed as a coating over existing structures in order to protect against weathering effects. It is ideal for anti-corrosion protection and is characterized by excellent mechanical properties and adhesion to various surfaces. Further development of this technology may allow obtaining new coatings with improved antistatic properties, which would be an excellent alternative compared to used antistatic epoxy paints. This paper will examine the influence of tetraalkylammonium salt (1), potassium hexafluorophosphate solution (2) and imidazolium-based ionic liquid (3) on the improvement of antistatic properties of the polyurea-polyurethane coatings. In addition, the modified samples were also verified in terms of changes in mechanical properties and the appearance of functional groups other than in the reference sample, as well as surface defects that may arise due to incompatibility of the antistatic additive with the polymer matrix. In order to obtain information about the properties mentioned above, the electrical resistance was determined, the tensile strength and elongation were measured, FT-IR spectra were made, and images were taken with the use of scanning electron microscopy. The conducted research showed that the antistatic properties of the tested hybrid coatings could be improved, but their use may be associated with certain limitations that should be taken into account when designing such materials.     

Targeting DNA Topoisomerase II in Antifungal Chemotherapy

Topoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand the range of therapeutic options. In this review paper, we discussed the usefulness of fungal topo II as a molecular target for new drug discovery. On the basis of previously published data, we described structural and biochemical differences between fungal and human enzymes as well as a molecular basis of differential sensitivity to known anticancer drugs targeting the latter. This review focuses especially on highlighting the differences that may underlie the selectivity of action of new inhibitors. Distinct sites within fungal topo II in comparison with human counterparts are observed and should be further studied to understand the significance of those sites and their possible usage in design of new drugs.     

Zinc–Cobalt Oxide Thin Films: High Curie Temperature Studied by Electron Magnetic Resonance

The material with a high Curie temperature of cobalt-doped zinc oxide embedded with silver-nanoparticle thin films was studied by electron magnetic resonance. The nanoparticles were synthesized by the homogeneous nucleation technique. Thin films were produced with the pulsed laser deposition method. The main aim of this work was to investigate the effect of Ag nanoparticles on the magnetic properties of the films. Simultaneously, the coexisting Ag⁰ and Ag²⁺ centers in zinc oxide structures are shown. A discussion of the signal seen in the low field was conducted. To analyze the temperature dependence of the line parameters, the theory described by Becker was used. The implementation of silver nanoparticles causes a significant shift of the line, and the ferromagnetic properties occur in a wide temperature range with an estimated Curie temperature above 500 K.     

Compositional control of electrical transport properties in the new series of defect thiospinels, Ga1−xGexV4S8−δ (0≤x≤1)

A new series of non-stoichiometric sulfides Ga_1−xGe_xV₄S_8−δ (0≤x≤1; δ≤0.23) has been synthesized at high temperatures by heating stoichiometric mixtures of the elements in sealed quartz tubes. The samples have been characterized by powder X-ray diffraction, SQUID magnetometry and electrical transport-property measurements. Structural analysis reveals that a solid solution is formed throughout this composition range, whilst thermogravimetric data reveal sulfur deficiency of up to 2.9% in the quaternary phases. Magnetic measurements suggest that the ferromagnetic behavior of the end-member phase GaV₄S₈ is retained at x≤0.7; samples in this composition range showing a marked increase in magnetization at low temperatures. By contrast Ga_0.25Ge_0.75V₄S_8−δ appears to undergo antiferromagnetic ordering at ca. 15 K. All materials with x≠1 are n-type semiconductors whose resistivity falls by almost six orders of magnitude with decreasing Ga content, whilst the end-member phase GeV₄S_8−δ is a p-type semiconductor. The results demonstrate that the physical properties are determined principally by the degree of electron filling of narrow-band states arising from intracluster V-V interactions.