Synthesis and evaluation of antitrypanosomal activity of some thiosemicarbazide derivatives of 1-butyl-6-fluoro-7-morpholino-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

The synthesis of thiosemicarbazide of 1-butyl-6-fluoro-7-morpholino-4-oxo-1,4-dihydroquinoline-3-carboxylic acid as well as its heterocyclic derivatives – 1,3,4-thiadiazole and 1,2,4-triazole are described; the modification of proper 1,2,4-triazole derivative by maleimides is also presented. Spectral properties of the prepared compounds and X-ray analysis for the selected compounds were studied. For the compounds antitrypanosomal potential and the toxicity were determined.     

Isomorphisms of Some Complex Poisson Brackets

Given a complex manifold M_i, structures of Poisson algebras on (M_i)=C(M_i,C) which are associated with a nondegenerate -closed (2,0)-form _i on M_i are considered. It is shown that every isomorphism of Poisson structures (M₁) (M₂) is generated by a biholomorphic map :M₂ M₁ such that ₂ = *₁     

Helical rosette nanotubes with tunable stability and hierarchy

The design of nanostructured materials with tunable dimensions and properties that maintain their structural integrity under physiological conditions is a major challenge in biomedical engineering and nanomedicine. Helical rosette nanotubes (HRN) are a new class of materials produced through a hierarchical self-assembly process of low molecular weight synthetic organic modules in water. Here, we describe a synthetic strategy to tune their stability and hierarchy by preorganization of the self-assembling units, control of net charge per unit of nanotube surface area, amphiphilicity, and number of H-bonds per self-assembling module, and through peripheral steric (de)compression. Using these criteria, HRNs with tunable stability and hierarchical architecture were produced from self-assembling modules that (a) persist as individual molecules in solution, (b) self-assemble into HRN but denature at high temperature (<85 degrees C), (c) self-assemble into HRN whose structural integrity persists even in boiling water (>95 degrees C), and (d) self-assemble into well-dispersed short nanotubes, long nanotubes, ribbons, or superhelices. Given the biocompatibility, synthetic accessibility, and chemical and physical tunability of these materials, numerous applications in biomedical engineering, materials science, and nanoscience and technology are envisioned.     

Tetrahydropyran-2,4-diones in the Synthesis of Fused N,O-Heterocycles

Condensation of 6-methyl(or phenyl)-tetrahydropyran-2,4-diones with 2-aminonaphthalene or 6-aminoquinoline and aromatic aldehydes in an aliphatic alcohol gave 5-aryl-2,2-dimethyl(or 2-phenyl)-1,2,5,6-tetrahydro-4H-benzo[f]pyrano[3,4-c]quinolin-4-ones and 5-aryl-2-methyl-1,2,5,6-tetrahydro-4H-pyrano[4,3-a][4,7]phenanthrolin-4-ones which are new N,O-heterocyclic systems containing fused aza- and diazaphenanthrene moieties and a 2-pyranone ring.     

Sequence selective hydrolysis of linear DNA using conjugates of Zr(IV) complexes and peptide nucleic acids

A series of conjugates of peptide nucleic acids (PNA) and Zr(IV) complexes was prepared. Their ability to hydrolyze DNA was tested using MALDI-TOF mass spectrometry and HPLC. The most efficient artificial restriction enzyme found, PNA conjugate with Zr(IV) complex of tris(hydroxymethyl)-aminomethane, cleaves DNA targets sequence selectively in close proximity to the Zr(IV) complex. It was demonstrated that cleavage products are substrates of terminal transferase.     

Synthesis, Structure and Selective Upper Rim Functionalization of Long Chained Alkoxythiacalix[4]arenes

The synthesis and X-ray structure investigation of the cone shaped monodecyloxythiacalix[4]arene, as well as the introduction of the reactive bromide or chloromethyl groups on it’s upper rim are described. Preparation of the amphiphilic derivative of thiacalixarene bearing three hydrophilic diethoxyphosphoryl groups at the upper rim and lipophilic decyloxy group at the lower rim is presented.     

Electromigration revisited: competition between Kirkendall shift and backstress in pure metals and two-phase alloys

The simple phenomenological model and analytical approach of electromigration in the two-phase alloy (solder) under combined influence of the Kirkendall effect, backstress and sedimentation is presented. It is compared with electromigration in pure metal under condition of quasi-equilibrium vacancies (unlimited power of vacancy sinks-sources) and electromigration in pure metal with account of nonequilibrium vacancies.     

A convenient synthesis method of 5-oxopyrazolo[4,3-b]pyridine-6-carboxylic acids and their nitriles

Chemistry of Heterocyclic Compounds - N-Boc-protected 5-formyl-1H-pyrazol-4-amines react with malonic acid in pyridine in the presence of pyrrolidine at 45–50°С or with malonic...     

Anisotropic Nucleation,Growth and Ripening under Stirring—A Phenomenological Model

The anisotropic formation of elongated metal-oxide aggregates in water under intensive stirring is analyzed. It is treated in terms of anisotropic ballistically mediated aggregation kinetics in open systems. The basic kinetic equations describing the stages of homogeneous nucleation, independent growth, and ripening of the aggregates are formulated for the open system under the external influence with the stirring intensity as the main parameter governing the process. The most significant elongation of the aggregates is shown to evolve at the ripening stage.     

Kinetics of ethanol decay in mouth‐ and nose‐exhaled breath measured on‐line by selected ion flow tube mass spectrometry following varying doses of alcohol

A study has been carried out of the decay of ethanol in mouth‐exhaled and nose‐exhaled breath of two healthy volunteers following the ingestion of various doses of alcohol at different dilutions in water. Concurrent analyses of sequential single breath exhalations from the two volunteers were carried out using selected ion flow tube mass spectrometry, SIFT‐MS, on‐line and in real time continuously over some 200 min following each alcohol dose by simply switching sampling between the two volunteers. Thus, the time interval between breath exhalations was only a few minutes, and this results in well‐defined decay curves. Inspection of the mouth‐exhaled and nose‐exhaled breath data shows that mouth contamination of ethanol diminished to insignificant levels after a few minutes. The detailed results of the analyses of nose‐exhaled breath show that the peak levels and the decay rates of breath ethanol are dependent on the ethanol dose and the volume of ethanol/water mixture ingested. From these data, both the efficiency of the first‐pass metabolism of ethanol and the indications of gastric emptying rates at the various doses and ingested volumes have been obtained for the two volunteers. Additionally and simultaneously, acetaldehyde, acetic acid and acetone were measured in each single breath exhalation. Acetaldehyde, the primary product of ethanol metabolism, is seen to track the breath ethanol. Acetic acid, a possible secondary product of this metabolism, was detected in the exhaled breath, but was shown to largely originate in the oral cavity. Breath acetone was seen to increase over the long period of measurement due to the depletion of nutrients. Copyright © 2010 John Wiley & Sons, Ltd.