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Query: UMLS:C0432222 (SEM)
 47,337 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of 2-amino-9-(3-acyloxymethyl-4-alkoxycarbonyloxybut-1-yl)purin es (1-8) and 2-amino-9-(3-alkoxycarbonyl-oxymethyl-4-alkoxycarbonyloxybut -1-yl)purines (9-12) were synthesized as potential prodrugs of penciclovir. Treatment of 6-deoxypenciclovir with trimethyl orthoacetate or triethyl orthopropionate (1.2 equiv) in DMF in the presence of p-TsOH.H2O (0.1 equiv) followed by quenching with excess H2O gave the corresponding mono-O-acetyl or mono-O-propionyl compound, 17 or 18, in excellent yields of 95 and 92%, respectively. Reactions of 17 or 18 with an appropriate alkyl (Me, Et, n-Pr, and i-Pr) 4-nitrophenyl carbonate (1.2 equiv) in pyridine in the presence of a catalytic amount of DMAP (0.1 equiv) at 80 degrees C afforded the monoacyl, monocarbonate derivatives of 6-deoxypenciclovir, 1-8, in 86 94% yields. Similar reactions of 6-deoxypenciclovir with 2.1 equiv of alkyl 4-nitrophenyl carbonate produced the dicarbonate derivatives 9 12 in 81-83% yields. Of the prodrugs tested in rats, 2-amino-9-(3-acetoxymethyl-4-isopropoxycarbonyloxybut-1-yl)purine (4) achieved the highest mean urinary recovery of penciclovir (36%), followed in order by compounds 2 (35%), 6 (35%), 7 (34%), 10 (34%), 8 (32%), 3 (32%), and famciclovir (31%). The mean urinary recovery of penciclovir and concentrations of penciclovir in the blood from 4 in mice were also slightly higher than those from famciclovir. The in vivo antiviral efficacy of 4 in HSV-1-infected normal BALB/c mice was higher than those of famciclovir and valaciclovir in terms of mortality (100, 80, and 40%) and mean survival time ( > 21, 13+/-5.0 (SEM), and 13+/-1.6 days). Compound 4 demonstrated an effective anti-hepadnaviral response with intrahepatic viral load being reduced by 90%, the viral supercoiled DNA levels reduced by 70% and Pre-S expression inhibited by 30% against duck hepatitis B virus (DHBV) in vivo, and did not cause any significant hepatotoxicity after 4 weeks of treatment.
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PMID:Synthesis and evaluation of 2-amino-9-(3-acyloxymethyl-4-alkoxycarbonyloxybut-1-yl)purines and 2-amino-9-(3-alkoxycarbonyloxymethyl-4-alkoxycarbonyloxybut-1- yl)purines as potential prodrugs of penciclovir. 1048 63

A new drug delivery formulation, biodegradable glycolic acid-lactic acid copolymer (PGLA) microspheres incorporating cisplatin (CDDP-MS) has been developed for the treatment of peritoneal carcinomatosis. Scanning electron microscopy showed that CDDP-MS has a smooth surface and few cisplatin crystals in the hollow. An electron probe micro analyzer revealed that cisplatin was located mainly in the matrix in the state of a molecule. Release profile in vitro of CDDP from microspheres showed that the initial burst was 21.2% and the remaining CDDP was released slowly thenceforth over 14 days. Hydrolysis of CDDP-MS progresses very slowly during the 14 days, but there was no morphological change in the SEM views. The dimethylformamide content entrapped within CDDP-MS, determined by a gas chromatography, was 136 ppm at the evaporation temperature of 47 degrees C. The 50% lethal dose value of CDDP-MS, calculated by the Litchfield-Wilcoxon method, was reduced to 57% of the cisplatin solution. Therapeutic experiment on mice with peritoneal carcinomatosis showed that CDDP-MS did not enhance therapeutic effect as compared with the same dose dosage of a cisplatin aqueous solution but large quantities of cisplatin could be given in case of CDDP-MS owing to less toxicity.
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PMID:Cisplatin incorporated in microspheres: development and fundamental studies for its clinical application. 1273 42

We describe the fabrication and characterization of tungsten oxide nanofibers using the electrospinning technique and sol-gel chemistry. Tungsten isopropoxide sol-gel precursor was incorporated into poly(vinyl acetate)(PVAc)/DMF solutions and electrospun to form composite nanofibers. The as-spun composite nanofibers were subsequently calcinated to obtain pure tungsten oxide nanofibers with controllable diameters of around 100 nm. SEM and TEM were utilized to investigate the structure and morphology of tungsten oxide nanofibers before and after calcination. The relationship between solution concentration and ceramic nanofiber morphology has been studied. A synchrotron-based in situ XRD method was employed to study the dynamic structure evolution of the tungsten oxide nanofibers during the calcination process. It has been shown that the as-prepared tungsten oxide ceramic nanofibers have a quick response to ammonia with various concentrations, suggesting potential applications of the electrospun tungsten oxide nanofibers as a sensor material for gas detection.
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PMID:Fabrication and characterization of polycrystalline WO3 nanofibers and their application for ammonia sensing. 1712 39

This study focuses on the adsorption properties of activated carbon nanofibers (CNFs) fabricated by electrospinning polyacrylonitrile solutions dissolved in dimethylformamide, followed by heat treatment at high activation temperatures (700, 750, 800 degrees C). The samples were characterized by BET, SEM, and XRD. In addition, the adsorption energy distribution functions of CNFs were analyzed by using the generalized nonlinear regularization method. Comparative analysis of energy distribution functions provided significant information on the energetic and structural heterogeneities of CNFs. Furthermore, an investigation of adsorption equilibrium and kinetics of methylene blue (MB) and congo red (CR) revealed that the adsorption capacity and kinetics of MB are much higher and faster than that of CR on a given sample. Our experimental and theoretical results suggest that the CNFs used in this work may be widely used as an adsorbent.
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PMID:Heterogeneous adsorption of activated carbon nanofibers synthesized by electrospinning polyacrylonitrile solution. 1725 15

Electrospun zein membranes were prepared using DMF as solvent. By changing the solution concentration, the electrospinning voltage and the distance between the spinneret and collector, nanofibrous meshes without bead defects could be obtained. In order to improve the mechanical strength of the hydrated zein meshes, core-shell-structured nanofibrous membranes with PCL as the core material and zein forming the shell were prepared by coaxial electrospinning. The core-shell structure of the composite fibers was confirmed by SEM characterization of the fibers, either extracted with chloroform to remove the inner PCL, or elongated to expose their cross-section. The composition and average diameter of the composite fibers could be modulated by the feed rate of the inner PCL solution. It was found that the core-shell fibrous membranes have similar wettability to the electrospun zein mesh. The presence of PCL in the fibers could significantly improve the mechanical properties of the zein membrane.
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PMID:Fabrication and characterization of zein-based nanofibrous scaffolds by an electrospinning method. 1742 29

We prepared buckypapers with surface densities in the 1.13-5.66 mg x cm(-2) range by filtering multi-wall carbon nanotube (MWCNT) suspensions in acetyl-acetone (acac) and dimethylformamide (DMF) through 0.45 microm nylon filters. Filtration curves were evaluated using the Carman equation. The average resistance of the filter itself was found to be Rm = 3.79 x 10(10) m(-1) for acac and 8.49 x 10(10) m(-1) for DMF The specific resistance a of the filter cakes decreased with increasing film surface density from 16.1 x 10(12) m x kg(-1) (for the 1.13 mg x cm(-2) film from DMF) to 4.38 x 10(12) m x kg(-1) (for the 5.66 mg x cm(-2) film from DMF). The effective diffusivity of N2 at 298 K and a pressure difference of 10 mbar was also determined for all membranes and found to fall into the 1.14 x 10(-9)-3.74 x 10(-9) m2 x s(-1) range. Both the porosity and the tortuosity of buckypapers increased with their thickness. An approx. 5 microm thick Teflon (PTFE) coating was applied to the MWCNT membranes by pulsed laser deposition. The gas permeability of the MWCNT-PTFE membranes matches that of the uncoated nanotube films. This observation is an agreement with our SEM and AFM data on porous coating morphology.
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PMID:Morphology and N2 permeability of multi-wall carbon nanotube--Teflon membranes. 1745 Sep 32

The treatment of a suspension of graphite oxide (GO) with sodium azide leads to a material that, after reduction, features amino groups at the top and bottom of the sheets. These groups react through microcontact printing with an isothiocyanate monolayer on a silicon oxide substrate to form covalent bonds that strongly attach to the particles on the surface. With ultrasonication it is possible to obtain exfoliation of the sheets that are not covalently bound to the surface leaving single-layer platelets attached to the substrate. The azido derivative can be also used to functionalize the graphene oxide with long alkylic chains through a click chemistry approach. This functionalization results in the exfoliation of this material in dimethylformamide. The novel materials were fully characterized by different techniques including IR spectroscopy, thermogravimetric analysis (TGA), scanning and transmission electron microscopy (SEM and TEM), X-Ray photoelectron spectroscopy (XPS), and solid state NMR spectroscopy. The material with amino groups, after the reduction step, is conductive with a resistivity only approximately seven times larger than that of unprocessed graphite. This implies that after reduction of the GO, the conjugated sp2 network is largely restored. We consider this to be an important step towards a chemical approach for forming conducting large-area platelet films of single-layer graphene.
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PMID:The formation of large-area conducting graphene-like platelets. 1960 86

Two functional ethynyl-pyrene derivatives have been designed and synthesized by di- and tetra-substitutions of bromo pyrene derivatives with N-(4-ethynylphenyl)-3,4,5-tris(hexadecyloxy)benzamide fragments. The photoluminescence wavelength of the pyrene core can be tuned by the substitution pattern and the state of matter (solid, solution, gel, or liquid crystal). The disubstituted pyrene derivative 1 is not mesomorphic but produces robust and highly fluorescent gels in DMF, toluene, and cyclohexane. The well-defined fibers and ropes of the gel states were characterized by SEM and laser scanning confocal microscopy, and extended over several micrometers. The gels were integrated as active layers in field-effect transistors, which provided good bulk electron and hole charge mobilities as well as light emission generation. The tetra-substituted pyrene derivative is not a gelator but displays a stable liquid crystalline phase with 2D hexagonal symmetry between 20 and 200 degrees C. The pronounced luminescence properties of the mesophase allow one to observe original mesophase textures with flower-like patterns directly by fluorescence microscopy without crossed-polarizers.
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PMID:Luminescent ethynyl-pyrene liquid crystals and gels for optoelectronic devices. 1992 2

The effects of the type of solvents on the aggregation behavior of poly(styrene-ran-methacrylic acid) (PSMAA) cast onto silicon wafer were studied using a SEM method. It was found that polystyrene prepared from DMF formed non-spherical aggregates but that PSMAA formed mixtures of ellipsoids and spheres. As the acid content increased, the spheres having a distinct boundary started contacting each other, and the average size of spherical particles decreased. Upon neutralization, the spherical particles became contacted spheres covered with much smaller spheres (ca. 20 nm in their sizes) and formed micro-gels. These results were compared to the data in the previous study of samples obtained from either water or THF. It was observed that the solubility parameters of the copolymers and ionomers, and polarity of solvents were some of key factors that determine the aggregation behavior of the polymers. The volatility of the solvent was also found to be an important factor for the aggregation behavior of polymers.
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PMID:Effects of the type of solvents on the morphology of styrene-methacrylic acid random copolymers cast onto silicon wafer. 2035 5

Understanding the mechanism of nanoparticle self-assembly is of critical significance for developing synthetic strategies for complex nanostructures. By encapsulating aggregates of Au nanospheres in shells of polystyrene-block-poly(acrylic acid), we prevent the dissociation and aggregation typically associated with the drying of solution samples on TEM/SEM substrates. In our study of the salt-induced aggregation of 2-naphthalenethiol-functionalized Au nanospheres in DMF, the trapping of the solution species under various experimental conditions permits new insights in the mechanism thereof. We provide evidence that the spontaneous linear aggregation in this system is a kinetically controlled process and hence the long-range charge repulsion at the "transition state" before the actual contact of the Au nanospheres is the key factor. Thus, the charge repulsion potential (i.e. the activation energy) a nanosphere must overcome before attaching to either end of a nanochain is smaller than attaching on its sides, which has been previously established. This factor alone could give rise to the selective end-on attachment and lead to the linear assembly of originally isotropic Au nanospheres.
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PMID:Mechanistic investigation into the spontaneous linear assembly of gold nanospheres. 2066 7


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