Abstract
We investigated the analgesic and antiemetic efficacy of gabapentin or ergotamine/caffeine (Cafergot), in addition to conservative treatment consisting of bed rest and adequate fluid intake, for the treatment of postdural puncture headache (PDPH).
In this randomized, prospective, con...
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PMID: 21536541
PDF is available here.
Abstract
We investigated the analgesic and antiemetic efficacy of gabapentin or ergotamine/caffeine (Cafergot), in addition to conservative treatment consisting of bed rest and adequate fluid intake, for the treatment of postdural puncture headache (PDPH).
In this randomized, prospective, con...
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PMID: 21536541
PDF is available here.
Abstract
A dual-catalysis approach enables the small-molecule catalyzed kinetic resolution of allylic amines by acylation. By employing 2 mol % of each 4-(pyrrolidino)pyridine (PPY) and a readily available chiral hydrogen-bonding cocatalyst, the first nonenzymatic kinetic resolution of allyli...
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PMID: 21476518
PDF is available here.
Abstract
We still need the newly more effective neuroprotective drugs which can be applied to many ischemic stroke patients. Therefore, we review and describe the future neuroprotective strategies in the post-thrombolysis era....
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PMID: 21706826
PDF is available here.
Abstract
Two novel, bionanocomposite scaffolds were evaluated in a rodent model over the course of three months to determine whether these scaffolds possessed adequate biocompatibility characteristics to warrant further evaluation as possible tissue reconstruction scaffolds. These bionanocomp...
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PMID: 21210516
PDF is available here.
Abstract
Silica and silicates are widely used in nanomedicine with applications as diverse as medical device coatings to replacement materials in tissue engineering. Although much is known about silica and its synthesis, relatively few biomedical scientists fully appreciate the link that exis...
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PMID: 21385130
PDF is available here.
Abstract
We describe a complementary technique in the library design process, termed ProSAR, to effectively cover the accessible pharmacophore space around a given scaffold. With this method reagents are selected such that each R-group on the scaffold has an optimal coverage of pharmacophoric features. This...
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PMID: 20981522
PDF is available here.
Abstract
We report our recent finding that these ligands decompose in situ to pyridine-2-carboxylic acid and its derivatives, in the presence of a manganese source, H(2)O(2) and a base. Importantly, the decomposition occurs prior to the onset of catalysed oxidation of organic substrates. It is found that the...
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PMID: 20886164
PDF is available here.
Abstract
At T≥ 140 °C, different primary aromatic amines (pX-C(6)H(4)NH(2); X = H, OCH(3), CH(3), Cl) react with both ethylene- and propylene-carbonates to yield a chemoselective N-alkylation process: bis-N-(2-hydroxyalkyl)anilines [pX-C(6)H(4)N(CH(2)CH(R)OH)(2); R = H, CH(3)] are the major products and t...
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PMID: 20844790
PDF is available here.
Abstract
A novel, practical and efficient enantioselective synthesis of sphingoid bases, l-threo-[2S,3S]-sphinganine (safingol), l-threo-[2S,3S]-sphingosine, l-arabino-[2R,3S,4R] and l-xylo-[2R,3S,4S]-C(18)-phytosphingosine is described. The synthetic strategy features the Sharpless kinetic resolution and te...
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PMID: 20844791
PDF is available here.
Aizhi Zhu,
Weiqiang Zhan,
Zhongxing Liang,
Younghyoun Yoon,
Hua Yang,
Hans E Grossniklaus,
Jianguo Xu,
Mauricio Rojas,
Mark Lockwood,
James P Snyder,
Dennis C Liotta and
Hyunsuk Shim
Abstract
The C-X-C chemokine receptor type 4 (CXCR4)/stromal cell derived factor-1 (SDF-1 or CXCL12) interaction and the resulting cell signaling cascade play a key role in metastasis and inflammation. On the basis of the previously published CXCR4 antagonist 5 (WZ811), a series of novel nonpeptidic anti-CXC...
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PMID: 21105715
PDF is available here.
Abstract
(103)Rhodium(III) complexes derived from seven acyclic tetradentate N(2)S(2) ligands (one diaminedithiol and six diaminedithioether ligands) have been synthesized and characterized. Structural variations in the ligand include the length of carbon backbone between the coordinating atoms (222; 232; 32...
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PMID: 20890539
PDF is available here.
Abstract
A long-chain amidoamine derivative (C18AA) acts as a normal organogelator in toluene, but changes to a heat-induced gelator, exhibiting a phase transition from sol to gel on heating upon addition of aqueous LiCl to the toluene gel. The thermal response of the heat-induced gel of C18AA was highly sen...
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PMID: 20865209
PDF is available here.
Abstract
An efficient tandem reaction system was developed, in which primary alcohols were used for the oxidation to the corresponding aldehydes followed by an asymmetric α-oxyamination with a resin-supported peptide catalyst.
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PMID: 20859596
PDF is available here.
Abstract
We report on the possibility of obtaining organic polymeric matrixes allowing the development of new high performance fire-resistant products by recycling downsized thermostable waste materials. Phenolic resins have been used as binders for recycled waste. Furthermore, considering that reinforced pl...
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PMID: 20605431
PDF is available here.
Abstract
SmI(2)/H(2)O promotes selective α-monodefluorinations, while addition of an amine results in complete α-defluorination reactions.
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PMID: 20838692
PDF is available here.
Abstract
A new strategy for the highly efficient one-pot synthesis of 3-amino-/alkylthio-cyclobut-2-en-1-ones based on the cyclization of acyl ketene dithioacetals is disclosed. In addition, the rearrangement of 3-amino-cyclobut-2-en-1-ones to 4-quinolone derivatives is described.
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PMID: 20838675
PDF is available here.
Abstract
Streptomyces sp. GF3587 and 3546 were found to be imine-reducing strains with high R- and S-selectivity by screening using 2-methyl-1-pyrroline (2-MPN). Their whole-cell catalysts produced 91 mM R-2-methylpyrrolidine (R-2-MP) with 99.2%e.e. and 27.5 mM S-2-MP (92.3%e.e.) from 2-MPN at 91-92% convers...
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PMID: 20820664
PDF is available here.
Abstract
A new, heterogeneous, 4 A molecular sieve-supported copper(ii) catalyst was developed and was used successfully in the A(3) coupling of alkynes, aldehydes and amines under simple reaction conditions.
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PMID: 20740243
PDF is available here.
Abstract
Condensation of an aldehyde with an α-amino-ester, followed by a tandem process involving cyclization to a seven-membered ring, deprotonation to an intermediate azomethine ylide and intramolecular dipolar cycloaddition gave tricyclic products related to stenine and neostenine.
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PMID: 20737084
PDF is available here.
Abstract
The first highly efficient Michael addition of challenging α,α-disubstituted aldehydes to maleimides catalyzed by a simple bifunctional primary amine thiourea catalyst/benzoic acid system has been successfully developed to generate quaternary carbon centers in high yields (up to 99%) with excellen...
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PMID: 20730207
PDF is available here.
Abstract
Five electroactive ferrocene tags for labelling of biomolecules are contrasted with regard to conjugation reactivity with amine and thiol moieties, stability to loss of electrochemical activity, and impact of molecular structure on the redox potential of the free and DNA-conjugated forms.
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PMID: 20740226
PDF is available here.
Abstract
The study examines the potential genotoxicity of three antiepileptic drugs (phenytoin sodium, pregabalin, gabapentin) using the wing somatic mutation and recombination test (SMART) in Drosophila melanogaster. Trans-heterozygous (two genetic markers mwh and flr) third-instar larvae of D. melanogaster...
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PMID: 20600525
PDF is available here.
Abstract
We systematically investigated cellular internalization, toxicity, and innate immune response of HNPs in human breast cancer (SK-BR-3) and mouse alveolar macrophage (J774A.1) cells. Size- and surface functionality-dependent cellular uptake of HNPs was investigated by fluorescence labeling (fluoresce...
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PMID: 20698555
PDF is available here.
Abstract
We acutely injected intrathecal ondansetron in rats between 14 and 30 days after SNL and assessed effects on thermal and mechanical hypersensitivity. We also determined the density of serotonergic nerve fibers, serotonin content and the levels of 5-HT3 receptors within the spinal cord at this time p...
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PMID: 20637741
PDF is available here.
Abstract
Chemoenzymatic dynamic kinetic resolution (DKR) of amines involving sulfanyl radical-induced racemization happened to be the very first switchable DKR process allowing the synthesis of either (R)- or (S)-amides, in good yield and high enantiomeric excess, depending on the nature of the enzyme; the d...
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PMID: 20661510
PDF is available here.
Abstract
A cascade aza-Michael-Henry-dehydration reaction catalyzed by quinidine-derived tertiary amine-thiourea catalyst was developed via installation of suitable electron withdrawing groups at the amino function of aniline. This strategy led to a one-step preparation of chiral 3-nitro-1,2-dihydroquinoline...
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PMID: 20648391
PDF is available here.
Abstract
We have investigated protic ionic liquids obtained by proton transfer from a common acid, acetic acid, to a range of amine bases of similar pK(a)(aq) values. Probe indicator observations, transport property data allowing the construction of Walden plots and computational studies all suggest that the...
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PMID: 20601995
PDF is available here.
Abstract
A highly enantioselective group 5 metal amide catalyst system is reported for the hydroaminoalkylation of secondary amines to give chiral amines in good yields with excellent ee values (up to 93%) by loading of 5% precatalyst.
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PMID: 20668747
PDF is available here.
Abstract
The benzoyl peroxide (BPO)-promoted oxidative functionalization of tertiary amines under transition-metal-free reaction conditions was developed. Various 1-trifluoromethylated tetrahydroisoquinoline derivatives were prepared by employing this method. It constitutes the first example of direct triflu...
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PMID: 20694243
PDF is available here.
Abstract
The direct alpha-cyanoamination of isatins using TMSCN has been developed, which is carried out in methanol without any catalyst. A new bifunctional cinchona alkaloid-based phosphinamide catalyst 7 could promote the Strecker reaction of isatins derived ketimine with TMSCN in up to 74% ee.
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PMID: 20617240
PDF is available here.
Abstract
A series of mixed ligand platinum(II) oxadiazoline complexes bearing 7-nitro-1,3,5-triazaadamantane (7-NO(2)TAA) as a labile and reactive nitrogen ligand has been synthesised from easily accessible starting materials. [2+3] cycloaddition of nitrones R(1)R(2)C-N(+)(Me)O(-) to only one of the nitrile...
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PMID: 20657943
PDF is available here.
Abstract
Peak plasma gabapentin concentration increased with increasing gabapentin dose. After administration of the 5, 10, and 30 mg/kg doses, median interval until the greatest gabapentin concentration was detected was 60, 120, and 90 minutes, respectively (interval ranges were 60 to 120 minutes, 60 to 120...
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PMID: 20807141
PDF is available here.
Abstract
A fast and convenient spectroscopic methodology to determine the water uptake capacity of amphiphile assemblies studied in multilayer films is presented. This method was developed to provide a reliable but relatively simple tool for estimating the binding potency of such complex systems. The water-b...
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PMID: 20635078
PDF is available here.
Abstract
We conclude that gabapentin did not have a detectable effect on the MAC of isoflurane in cats....
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PMID: 20547821
PDF is available here.
Abstract
Primary aliphatic biogenic amines have been successfully oxidized using a quinonoid species that mimics the metabolic activity of copper-containing amine oxidase (CuAO) enzymes. Especially, high catalytic performances were observed with aminoacetone, a threonine catabolite, and methylamine, a metabo...
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PMID: 20574584
PDF is available here.
Abstract
The N-(pyrrolidin-2-ethyl) glycine-based PNA (pet-PNA) backbone, with 4-amino or 4-guanidino-functionalized pyrrolidine ring, confers constrained conformational flexibility on aegPNA. The oligomers bind to the target DNA and RNA sequences with increased sequence specificity and antiparallel versus p...
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PMID: 20539879
PDF is available here.
Abstract
An original high-performance liquid chromatographic method with fluorescence detection is presented for the simultaneous determination of the three antiepileptic drugs gabapentin, vigabatrin and topiramate in human plasma. After pre-column derivatisation with dansyl chloride, the analytes were separ...
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PMID: 20363577
PDF is available here.
Abstract
Three-component reactions with 3,4-diiodoalk-2-enoic derivatives, primary amines, and terminal alkynes proceeded to give trisubstituted pyrroles in fair to good yields in the presence of palladium and copper catalysts under mild reaction conditions.
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PMID: 20532274
PDF is available here.
Abstract
Complexes [Re(CO)(3)(N-RIm)(3)]OTf (N-RIm=N-alkylimidazole, OTf=trifluoromethanesulfonate; 1a-d) have been straightforwardly synthesised from [Re(OTf)(CO)(5)] and the appropriate N-alkylimidazole. The reaction of compounds 1a-d with the strong base KN(SiMe(3))(2) led to deprotonation of a central C-...
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PMID: 20572178
PDF is available here.
Christopher K Savile,
Jacob M Janey,
Emily C Mundorff,
Jeffrey C Moore,
Sarena Tam,
William R Jarvis,
Jeffrey C Colbeck,
Anke Krebber,
Fred J Fleitz,
Jos Brands,
Paul N Devine,
Gjalt W Huisman and
Gregory J Hughes
Abstract
We report an efficient biocatalytic process to replace a recently implemented rhodium-catalyzed asymmetric enamine hydrogenation for the large-scale manufacture of the antidiabetic compound sitagliptin. Starting from an enzyme that had the catalytic machinery to perform the desired chemistry but lac...
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PMID: 20558668
PDF is available here.
Abstract
We previously investigated bladder cancer risk in a cohort of dyestuff workers who were heavily exposed to aromatic amines from 1922 through 1972. We updated the follow-up by 14 years (through 2003) for 590 exposed workers to include more than 30 years of follow-up since last exposure to aromatic am...
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PMID: 20548022
PDF is available here.
Abstract
Well-defined AB2 Y-shaped miktoarm star copolymers of PNIPAM-b-(PZLL)2 and PNIPAM-b-(PLL)2 were synthesized through the combination of atom transfer radical polymerization (ATRP), ring-opening polymerization (ROP), and click chemistry, where PNIPAM, PZLL, and PLL are poly(N-isopropylacrylamide), pol...
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PMID: 20536122
PDF is available here.
Abstract
The aim of this work is to construct a safe and effective drug candidate against Streptococcus suis infection. A panel of chitosan-based polymer conjugates with branched galabiose (Galalpha1-4Gal) side chains was synthesized as inhibitors of S. suis adhesion. The synthesis was achieved by using an a...
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PMID: 20540558
PDF is available here.
Abstract
A 3-compartment model with elimination from the central compartment best described the disposition of gabapentin administered IV to cats, but a 1-compartment model best described the disposition of gabapentin administered orally to cats. After IV administration, the mean +/- SEM apparent volume of t...
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PMID: 20594085
PDF is available here.
Abstract
We registered a worsening of hiccups.Responses were observed in 32 patients (74.4%) with gabapentin at a dosage of 900 mg/d and in 9 patients (20.93%) at 1200 mg/d.In 2 patients (4.65%), grade 2 sleepiness was observed and in 10 patients (23.25%), grade 1 sleepiness was observed based on the Epworth...
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PMID: 20414106
PDF is available here.
Abstract
We systematically quantified surface complexation of Np(V) onto whole cells, cell wall, and extracellular polymeric substances (EPS) of Shewanella alga strain BrY. We first performed acid and base titrations and used the mathematical model FITEQL to estimate the concentrations and deprotonation cons...
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PMID: 20521812
PDF is available here.
Abstract
It has been recently observed that small fibre neuropathy (SFN) may present as distal symmetrical polyneuropathy and with atypical non-length-dependent pattern.
To describe a small series of patients with non-length-dependent SFN, investigating corneal innervation wit...
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PMID: 20581138
PDF is available here.
Abstract
We show that activation of amines and nitroalkanes with an electrophilic iodine source can lead directly to amide products. Preliminary observations support a mechanism in which the polarities of the two reactants are reversed (German, umpolung) during carbon-nitrogen bond formation relative to trad...
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PMID: 20577205
PDF is available here.
Abstract
Many amines are proven or suspected to be carcinogenic and have been implicated in inducing cancer of the bladder. Therefore, the monitoring of their levels in environmental samples is important for the protection of health and the environment. Herein, a novel method for effective immobilization of...
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PMID: 20484789
PDF is available here.
Abstract
In this work, a reliable simple method has been introduced for predicting enthalpy of melting of nitroaromatic energetic compounds through their molecular structures. This method can be used for a wide range of nitroaromatics including halogenated nitroaromatic compounds. The contribution of hydroge...
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PMID: 20117881
PDF is available here.
Abstract
Polyethylene terephthalate (PET) waste flakes were degraded with aqueous methylamine and aqueous ammonia, respectively at room temperature in the presence and absence of quaternary ammonium salt as a catalyst for different periods of time. The aminolysed and ammonolysed PET samples were investigated...
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PMID: 20153927
PDF is available here.
Abstract
Solvent bar microextraction (SBME) combined with gas chromatography-flame ionization detector (GC-FID), was used for preconcentration and determination of some aliphatic amines in waste water samples. The effect of different variables on the extraction efficiency was studied simultaneously using an...
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PMID: 20202751
PDF is available here.
Abstract
We report that gabapentin is a good adjunct for visceral pain in a porphyria patient. CASE REPORT: A young female was admitted due to acute abdomen. On admission, she was noted to have hyponatremia, tachycardia, and hypertension. Then, she had episodes of seizure and confusion. Gabapentin was prescr...
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PMID: 20714961
PDF is available here.
Abstract
The synthesis, structure elucidation and antitumoral activity of novel heterocyclic compounds containing a carbazole nucleus are reported. Oxazinocarbazoles were synthesized by application of the Mannich reaction to the corresponding hydroxylated derivatives leading to 41 new molecules. Their cytoto...
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PMID: 20236739
PDF is available here.
Abstract
Fluorinated derivatives of 1,4-naphthoquinone are highly potent inhibitors of Cdc25A and Cdc25 phosphatases and growth of tumor cells. Five new N-substituted polyfluorinated derivatives of 2-amino-1,4-naphthoquinone were synthesized and their mutagenic and antioxidant properties in Salmonella cells,...
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PMID: 20189692
PDF is available here.
Abstract
Pain after movement was reduced by gabapentin from the second to tenth postoperative day and venlafaxine group in the last 3 days but no difference was found between the groups regarding pain during rest. Gabapentin reduced morphine consumed in the first 24 hours postoperatively. The analgesic requi...
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PMID: 20473044
PDF is available here.