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Hemagglutinating activity was studied in homogenates of three embryonic stages, and in the hemolymph of most instar larvae and in adult insects of Panstrongylus megistus, an important Chagas' disease vector in Brazil. A hemolymph lectin from the 5th instar larvae of P. megistus was purified through a biospecific adsorption by using formaldehyde-treated erythrocytes. The lectin fraction was desorbed with 0.2M D-galactose in 0.15M NaCl. The lectin fraction activity was inhibited by L-rhamnose, D-lactose, raffinose, D-galactose, and D-fucose. The electrophoretic pattern to native and acidic proteins resolved lectin fraction in two main bands with lectin activity. These bands were considered as multiple molecular forms or isoforms of P. megistus lectin. Under denaturating conditions, isoform 1 showed one band with apparent mol wt (MW) of 64 kDa while isoform 2 was resolved in two bands with MW of 64 and 33 kDa.  相似文献   
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New thieno[2,3-b]pyridine phosphoramidates compounds were synthesized and characterized by infrared; 1H, 13C, and 31P NMR spectroscopy; and high-resolution mass spectrometry. The products were obtained in good yields (64–82%) under mild conditions by nucleophilic aromatic substitution reaction of aminoalkylphosphoramidates over 4-chlorothieno[2,3-b]pyridine-5-carbonitrile. The crystal structures of two compounds were solved by x-ray diffraction and showed a network of intermolecular interactions involving phosphoramidate groups. Druglike properties and toxicity of the new compounds were studied with the help of the software Molinspiration, Osiris, and Toxtree, and were compared with the standard drugs amphotericin B, miltefosine, benznidazole, and nifurtimox.

[Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.]  相似文献   
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Regioselective synthesis of haloaromatic tertiary alcohols can be achieved by ortho deprotonation/electrophilic reactions of (η6- fluoroarene)Cr(CO)3 complexes with halobenzophenones and metal removal. The coexistence of different halogens in the aromatic rings of these molecules make them unique within the group of tertiary alcohols.  相似文献   
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Herein, we used tri-ureasil organic–inorganic hybrid material (tU5000) in order to enhance the solubility of nonsteroidal anti-inflammatory drugs and fine tuning the drug delivery profile. For the first time, we used tU5000 as a film-forming agent in order to provide an alternative vehicle for transdermal drug delivery systems which the cell viability of practically 100 % for the highest and the lowest tested concentrations of pure tU5000 indicated that the material was not cytotoxic. The physicochemical properties of the tU5000 drug carrier and drug-loaded hybrids were systematically studied using powder X-ray diffraction, differential scanning calorimetry, small-angle X-ray scattering, and Fourier-transform infrared spectroscopy. The structural changes of tU5000 as well as the relationships between the drug content and in vitro drug release behaviors were investigated. The results showed that the ibu molecules were homogeneously distributed in the tU5000 xerogels contributing to fine-tuning the drug delivery profile. Considering the ability to incorporated high drug content, simple and mild preparation procedure by one-pot sol–gel route, high stability of the materials, sustained-release property, this class of hybrid based on polymers and inorganic compounds may have potential applications in the design of pharmaceutical formulation as ophthalmic (contact lenses), transdermal (patches) and implantable (soft tissue) drug delivery systems.  相似文献   
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We investigate the relativistic and non-relativistic quantum dynamics of a neutral spin-1/2 particle subject to an external electromagnetic field in the presence of a cosmic dislocation. We analyze the explicit contribution of the torsion in the geometric phase acquired in the dynamics of this neutral spinorial particle. We discuss the influence of the torsion in the relativistic geometric phase. Using the Foldy–Wouthuysen approximation, the non-relativistic quantum dynamics is studied and the influence of the torsion on the Aharonov–Casher and He–McKellar–Wilkens effects are discussed. An erratum to this article can be found at  相似文献   
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A numerical method used for solving a two-phase flow problem as found in typical oil recovery is investigated in the setting of physics-based two-level operator splitting. The governing equations involve an elliptic differential equation coupled with a parabolic convection-dominated equation which poses a severe restriction for obtaining fully implicit numerical solutions. Furthermore, strong heterogeneity of the porous medium over many length scales adds to the complications for effectively solving the system. One viable approach is to split the system into three sub-systems: the elliptic, the hyperbolic, and the parabolic equation, respectively. In doing so, we allow for the use of appropriate numerical discretization for each type of equation and the careful exchange of information between them. We propose to use the multiscale finite volume element method (MsFVEM) for the elliptic and parabolic equations, and a nonoscillatory difference scheme for the hyperbolic equation. Performance of this procedure is confirmed through several numerical experiments.  相似文献   
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