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Direct Route (direct + route)
Selected AbstractsA Direct Route to 2-(,-D-Ribofuranosylthio)pyridine Glycosides.CHEMINFORM, Issue 10 2003Galal H. Elgemeie No abstract is available for this article. [source] In vivo functions of the prolyl-4-hydroxylase domain oxygen sensors: direct route to the treatment of anaemia and the protection of ischaemic tissuesACTA PHYSIOLOGICA, Issue 4 2009D. M. Katschinski Abstract The prolyl-4-hydroxylase domain (PHD) 1,3 enzymes have been identified based on their ability to regulate the stability of hypoxia-inducible factor , subunits and thus to modify hypoxia-inducible gene expression. Transgenic mouse models provided insights into the isoform-specific functions of these oxygen sensors with physiological implications for angiogenesis, erythropoiesis/oxygen transport, cardiovascular function, metabolism and tissue homeostasis. This knowledge is important for the ongoing development of small molecule PHD inhibitors that are currently tested in preclinical and clinical trials for the treatment of anaemia and for cytoprotection. This review aims at summarizing the insights obtained from key mouse knock-out models as well as first experiences in the therapeutic application of PHD inhibitors. [source] Asymmetric Aza-Morita,Baylis,Hillman Reactions of Alkyl Vinyl Ketones with N -Protected Imines or In Situ Generated N -Protected IminesEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 21 2010Xiao-Yang Guan Abstract DABCO-catalyzed aza-MBH reactions of N -Boc imines with MVK and EVK have been thoroughly investigated in the paper. The asymmetric version of this aza-MBH reaction was also systematically investigated by using a chiral amine or a chiral phosphane catalyst. It was found that most of the N -protected imines are suitable substrates under the mild reaction conditions and are able to give the corresponding adducts in moderate yields with high ee values. The TQO- or LB1-catalyzed aza-MBH reactions of N -protected ,-amidoalkyl phenyl sulfones or ,-amidoalkyl p -tolyl sulfones with MVK could be well conducted, which provides a facile and direct route to obtain highly enantioselective aza-MBH adducts. The Boc protecting group of the aza-MBH product could be easily removed under acidic conditions to give the corresponding ,-methylene-,-amino ketone or ,-methylene-,-amino alcohol derivatives in good yields. [source] New Solutions to the C-12,13 Stereoproblem of Epothilones B and D; Synthesis of a 12,13-Diol-Acetonide Epothilone B AnalogEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 15 2006Tanja Gaich Abstract New approaches are described to the synthesis of epothilone B and a 12,13-diol-acetonide derivative. Specifically the (12Z) double bond is formed quantitatively by a silicon-tethered ring-closing metathesis (RCM) reaction with 85,% selectivity. Alternatively, a direct route to the 12,13-epoxide by cyclization of a 12,13-diol has been developed. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006) [source] Optimization of tree-shaped flow distribution structures over a disc-shaped areaINTERNATIONAL JOURNAL OF ENERGY RESEARCH, Issue 8 2003S. Lorente Abstract In this paper, we review the fundamental problem of how to design a flow path with minimum overall resistance between one point (O) and many points situated equidistantly on a circle centred at O. This is a fundamental problem in energy engineering: the distribution of fluid, energy, electric power, etc., from points to surrounding areas. This problem is also fundamental in heat transfer and electronics cooling: how to bathe and cool with a single stream of coolant a disc-shaped area or volume that generates heat at every point. This paper outlines, first, a direct route to the construction of effective tree-shaped flow structures. The starting point is the optimization of the shape of each elemental area, such that the length of the flow path housed by the element is minimized. Proceeding towards larger and more complex structures,from elements to first constructs, second constructs, etc.,the paper develops tree-shaped flow structures between one point and a straight line, as an elemental problem, and a circle and its centre. We also consider the equivalent tree-shaped networks obtained by minimizing the pressure drop at every step of the construction, in accordance with geometric constraints. The construction method is applied to a fluid flow configuration with laminar fully developed flow. It is shown that there is little difference between the two methods. The minimal-length structures perform very close to the fully optimized designs. These results emphasize the robustness of optimized tree-shaped flows. Copyright © 2003 John Wiley & Sons, Ltd. [source] An Organocatalytic Domino Thia-Michael/Aldol Condensation Reaction: Highly Enantioselective Synthesis of Functionalized DihydrothiophenesADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 13 2010Jie Tang Abstract An organocatalytic domino thia-Michael/aldol condensation reaction of ,, ,-unsaturated aldehydes with 1, 4-dithiane-2,5-diol catalyzed by chiral diphenylprolinol TMS ether has been developed, which provides a new practical and direct route to chiral dihydrothiophenes with high yields (up to 90%) and excellent enantioselectivities (up to>99% ee). The catalytic mechanism of the domino reaction was further confirmed through the APCI-MS detection of proposed reaction intermediates. [source] Logarithmic perturbation theory for a spiked oscillator and sum rulesINTERNATIONAL JOURNAL OF QUANTUM CHEMISTRY, Issue 1 2005S. K. Bandyopadhyay Abstract We show that logarithmic perturbation theory nicely yields the wavefunction correction terms in closed forms for the spiked perturbation ,/x2 on the first excited state of the harmonic oscillator, where the conventional Rayleigh-Schrödinger scheme is known to encounter serious problems. The study also provides a direct route to obtain several sum rules, some of which appear to be new. © 2005 Wiley Periodicals, Inc. Int J Quantum Chem, 2005 [source] One-Pot Synthesis of Highly Substituted Allenylidene Derivatives via Palladium- or Nickel-Catalyzed Tandem Michael Addition,Cyclization ReactionADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 1-2 2009Yun Shi Abstract A simple and tandem synthetic approach, which offers an efficient, direct route to highly substituted indenes, has been developed by palladium- or nickel-catalyzed cyclization of propargylic compounds and nitrogen nucleophiles. The reaction takes place under mild conditions, and a possible mechansim is proposed. [source] An efficient one-pot synthesis of 6-aryl-5-cyano-2-thiopyrimidinone derivatives and their piperidinium ionic forms, x-ray crystal structuresJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 4 2006Saeed Balalaie Three-component condensation of benzaldehyde derivatives, alkyl cyanoacetates and thiourea in the presence of piperidine in reflux condition provides a direct route to piperidinium 6-aryl-5-cyano 2-thiopyrimidonate salts in good yields. These reactions were also carried out under microwave irradiation. The yields of products under the microwave condition were better as compared to the reflux media. The acidification of these ionic forms resulted in the formation of 6-aryl-5-cyano-2-thiopyrimidone derivatives. The X-ray structures of the ionic forms (4, 5, and 7) show that there are anionic thiopyrimidinone skeletons hydrogen bridged with piperidinium cations. [source] Hypothalamic Control of Anterior Pituitary Function: A HistoryJOURNAL OF NEUROENDOCRINOLOGY, Issue 6 2008H. Charlton The concept of neurohumoral control of anterior pituitary function championed by Geoffrey Harris was based upon clinical and biological observation backed by rigorous experimental testing. The areas of the brain involved in the control of gonadotrophic hormone synthesis and release were identified by electrical stimulation, lesioning and fibre tract cutting. The medial preoptic area (MPOA) proved to be a major integrating centre, with axon terminals from this region terminating at the median eminence releasing factors into the portal vessels to give a direct route from brain to pituitary. It took over a decade before the gonadotrophic hormone-releasing hormone (GnRH) was isolated, sequenced and synthesised. With antibodies raised against this peptide, the MPOA was identified as a site rich in GnRH neurones and the hormone was detected at high levels in portal blood extracts. A natural knockout of the GnRH gene was discovered in a hypogonadal (hpg) mouse. Hormone injections, gene replacement methods and neural grafting in these mutants all confirmed the central role of GnRH in reproduction. The modern techniques of molecular biology have allowed us to extend our knowledge base. In the last few years the role of kisspeptin and its receptor (GPR54) in the control of the GnRH neurone has added a further level of hypothalamic involvement in the modulation of reproduction. [source] Commercial Exploration of High-Temperature SuperconductivityLASER TECHNIK JOURNAL, Issue 4 2010Excimer Lasers Enable Novel Coated Superconductor Cylinders Superconductivity, which is the condition in which the electrical resistance of a material drops to zero, was discovered nearly 100 years ago. Since that time, large superconducting magnets such as those used in magnetic resonance imaging (MRI), nuclear magnetic resonance (NMR) and big physics experiments have been developed and can now be regarded as being commercial products extending our capabilities in medicine and science. Yet many industrial applications of high temperature superconductivity (HTS) are on the horizon waiting to enter the marketplace. Currently, numerous manufacturers are working on improving and upscaling HTS materials, which operate at liquid nitrogen temperatures, and the most promising configuration for these materials is in the form of long tapes also known as coated conductors. These coated conductors are wound into coils in order to produce electrical components such as motors, magnets, transformers etc. Depending on the component to be made, there is an alternative to fabricating long unit lengths of superconducting tape, and in forming stable robust windings utilizing them. Now, a new technique has been developed which is using pulsed laser deposition (PLD) to deposit a series of layers of superconducting material directly on to the surface of a cylinder and patterning them into coils. This configuration provides a very direct route for the production of components that conventionally involve winding processes. This article explores how coated conductor cylinders can be produced utilizing this technique and explains why industriallyproven excimers represent the optimum choice of laser source for this emergingtechnology. [source] Alterations in Taxol Production in Plant Cell Culture via Manipulation of the Phenylalanine Ammonia Lyase PathwayBIOTECHNOLOGY PROGRESS, Issue 6 2002Michelle C. Brincat One approach to increasing secondary metabolite production in plant cell culture is to manipulate metabolic pathways to utilize more resources toward production of one desired compound or class of compounds, such as diverting carbon flux from competing secondary pathways. Since phenylalanine provides both the phenylisoserine side chain and the benzoyl moiety at C-2 of Taxol, we speculated that blockage of the phenylpropanoid pathway might divert phenylalanine into Taxol biosynthesis. We used specific enzyme inhibitors to target the first enzyme in the phenylpropanoid pathway, phenylalanine ammonia lyase (PAL), the critical control point for conversion of l -phenylalanine to trans -cinnamic acid. Cinnamic acid acted quickly in reducing PAL activity by 40,50%, without affecting total protein levels, but it generally inhibited the taxane pathway, reducing Taxol by 90% of control levels. Of the taxanes produced, 13-acetyl-9-dihydro-baccatin III and 9-dihydrobaccatin III doubled as a percentage of total taxanes in C93AD and CO93P cells treated with 0.20 and 0.25 mM cinnamic acid, when all other taxanes were lowered. The PAL inhibitor ,-aminooxyacetic acid (AOA) almost entirely shut down Taxol production at both 0.5 and 1.5 mM, whereas l -,-aminooxy-,-phenylpropionic acid (AOPP) had the opposite effect, slightly enhancing Taxol production at 1 ,M but having no effect at 10 ,M. The discrepancy in the effectiveness of AOA and AOPP and the lack of effect with addition of phenylalanine or benzoic acid derivatives further indicates that the impact of cinnamic acid on Taxol is related not to its effect on PAL but rather to a specific effect on the taxane pathway. On the basis of these results, a less direct route for inhibiting the phenylpropanoid pathway may be required to avoid unwanted side effects and potentially enhance Taxol production. [source] Facile High-Yield Synthesis of Polyaniline Nanosticks with Intrinsic Stability and Electrical ConductivityCHEMISTRY - A EUROPEAN JOURNAL, Issue 33 2008Xin-Gui Li Prof. Abstract Chemical oxidative polymerization at 15,°C was used for the simple and productive synthesis of polyaniline (PAN) nanosticks. The effect of polymerization media on the yield, size, stability, and electrical conductivity of the PAN nanosticks was studied by changing the concentration and nature of the acid medium and oxidant and by introducing organic solvent. Molecular and supramolecular structure, size, and size distribution of the PAN nanosticks were characterized by UV/Vis and IR spectroscopy, X-ray diffraction, laser particle-size analysis, and transmission electron microscopy. Introduction of organic solvent is advantageous for enhancing the yield of PAN nanosticks but disadvantageous for formation of PAN nanosticks with small size and high conductivity. The concentration and nature of the acid medium have a major influence on the polymerization yield and conductivity of the nanosized PAN. The average diameter and length of PAN nanosticks produced with 2,M HNO3 and 0.5,M H2SO4 as acid media are about 40 and 300,nm, respectively. The PAN nanosticks obtained in an optimal medium (i.e., 2,M HNO3) exhibit the highest conductivity of 2.23,S,cm,1 and the highest yield of 80.7,%. A mechanism of formation of nanosticks instead of nanoparticles is proposed. Nanocomposite films of the PAN nanosticks with poly(vinyl alcohol) show a low percolation threshold of 0.2,wt,%, at which the film retains almost the same transparency and strength as pure poly(vinyl alcohol) but 262,000 times the conductivity of pure poly(vinyl alcohol) film. The present synthesis of PAN nanosticks requires no external stabilizer and provides a facile and direct route for fabrication of PAN nanosticks with high yield, controllable size, intrinsic self-stability, strong redispersibility, high purity, and optimizable conductivity. [source] Straightforward Synthesis of (R)-(,)-KjellmanianoneCHEMISTRY - A EUROPEAN JOURNAL, Issue 4 2004Jens Christoffers Prof. Dr. Abstract A direct route to enantiomerically pure (,)-kjellmanianone is reported. The synthesis involves a cerium-catalyzed ,-hydroxylation and an enzyme-catalyzed procedure to resolve tertiary alcohols at key stages. The intermediate ,-oxo ester was ,-hydroxylated to give good yields of racemic kjellmanianone. The resolution of the racemic material was achieved by enzymatic saponification, followed by a chemical decarboxylation sequence to give enantiopure (,)-kjellmanianone with 99,% ee. Bromination then afforded the (,)-bromo derivative, whose X-ray structure provided evidence for the R configuration of (,)-kjellmanianone. [source] Developmental neural plasticity and its cognitive benefits: olivocerebellar reinnervation compensates for spatial function in the cerebellumEUROPEAN JOURNAL OF NEUROSCIENCE, Issue 5 2007Melina L. Willson Abstract The adult mammalian central nervous system displays limited reinnervation and recovery from trauma. However, during development, post-lesion plasticity may generate alternative paths, thus providing models to investigate reinnervation and repair. After unilateral transection of the neonatal rat olivocerebellar path (pedunculotomy), axons from the remaining inferior olive reinnervate the denervated hemicerebellum. Unfortunately, reinnervation to the cerebellar hemisphere is incomplete; therefore, its capacity to mediate hemispheric function (navigation) is unknown. We studied sensorimotor control and spatial cognition of rats with and without transcommissural reinnervation using simple (bridge and ladder) and complex (wire) locomotion tests and the Morris water maze (hidden, probe and cued paradigms). Although pedunculotomized animals completed locomotory tasks more slowly than controls, all groups performed equally in the cued maze, indicating that lesioned animals could orientate to and reach the platform. In animals pedunculotomized on day 3 (Px3), which develop olivocerebellar reinnervation, final spatial knowledge was as good as controls, although they learned more erratically, failing to retain all information from one day to the next. By contrast, animals pedunculotomized on day 11 (Px11), which do not develop reinnervation, did not learn the task, taking less direct routes and more time to reach the platform than controls. In the probe test, control and Px3, but not Px11, animals swam directly to the remembered location. Furthermore, the amount of transcommissural reinnervation to the denervated hemisphere correlated directly with spatial performance. These results show that transcommissural olivocerebellar reinnervation is associated with spatial learning, i.e. even partial circuit repair confers significant functional benefit. [source] | |||||||||||||