排序方式: 共有22条查询结果,搜索用时 15 毫秒
1.
Emtenäs H Carlsson M Pinkner JS Hultgren SJ Almqvist F 《Organic & biomolecular chemistry》2003,1(8):1308-1314
Optically active bicyclic beta-lactams were synthesized, starting from 2-H-delta 2-thiazolines and Meldrum's acid derivatives. Several methods to accomplish an ester hydrolysis without damaging the beta-lactam framework were investigated. A rapid CsOH saponification of the beta-lactam methyl esters was developed and protonation of the Cs-carboxylates by Amberlite (IR-120 H+) afforded a series of bicyclic beta-lactam carboxylic acids. Moreover, a convenient method for the synthesis of 2-H-delta 2-thiazolinecarboxylic acid methyl ester 2 was developed. Bicyclic beta-lactam carboxylic acids 7a-g and aldehydes 4a-d were screened for their affinity to the bacterial periplasmic chaperone PapD using a surface plasmon resonance technique. beta-Lactams substituted with large acyl substitutents showed better binding to the chaperone than the native C-terminal peptide PapG 8, demonstrating that bicyclic beta-lactams constitute a new class of potential bacterial chaperone inhibitors. 相似文献
2.
Emtenäs H Ahlin K Pinkner JS Hultgren SJ Almqvist F 《Journal of combinatorial chemistry》2002,4(6):630-639
A new method for the solid-phase synthesis of enantiomerically enriched highly substituted ring-fused 2-pyridinones 13 has been developed. The synthesis mediates introduction of substituents at two positions in the 2-pyridinone ring in a diverse manner and is suitable for parallel synthesis. (19)F NMR spectroscopy was used as a tool to monitor each of the five steps in the reaction sequence. The optimized conditions thus obtained were then used to prepare a library of 20 2-pyridinones with high yields. The library members were chosen from a statistical multivariate design to ensure diversity and reliable data for structure-activity relationships. Screening of the library against the bacterial periplasmic chaperone PapD was performed using surface plasmon resonance. Three new 2-pyridinones with a higher affinity for the chaperone PapD than the previous best 13[10,1] were found, and important structural features could be deduced. 相似文献
3.
We use tools of the equilibrium statistical mechanics of disordered systems to study analytically the statistical properties of an ecosystem composed of N species interacting via random mutual interactions, as well as via deterministic self-interactions of order p>/=2. We show that the main effect of increasing the order of the interactions among the species is to make the system less competitive, in the sense that the fraction of extinct species is greatly reduced. In addition, we find that for p>2 there is a threshold value which gives a lower bound to the concentration of the surviving species, preventing then the existence of rare species and, consequently, increasing the robustness of the ecosystem to external perturbations. 相似文献
4.
In this paper, the long-run dynamics of a resonant converter is studied. The modelling of the resonant converter can be done using various approximations and the long-run dynamics of the two dimensional cases were earlier analysed. In this paper, we discuss results that can be extended to the three dimensional case. It seems that limit cycles describe the long-run dynamics in important situations in the three dimensional case, too. Our objective is to relate the limit cycles found previously in the two-dimensional case to those found now in the three dimensional approximation. 相似文献
5.
Rüther T Hultgren VM Timko BP Bond AM Jackson WR Wedd AG 《Journal of the American Chemical Society》2003,125(33):10133-10143
Oxidative photocurrents measured upon irradiation by a 7-W visible light (wavelength 312-700 nm) demonstrated that the sulfo-polyoxometalate anion clusters [S2W18O62]4- (1a), [S2Mo18O62]4- (1b), and [SMo12O40]2- (2) may be activated photochemically to oxidize the organic substrates benzyl alcohol, ethanol, and (-)-menthol. In the case of catalytic photooxidation of benzyl alcohol to benzaldehyde in the presence of 1a, quantitative electrochemical methods have identified pathways for the oxidation of reduced forms of 1 generated during the catalysis. More generally, the oxidation pathways P(n+2)- + 2H+ <==> Pn- + H2 and 2P(n+2)- + O2 + 4H+ <==> 2Pn- + 2H2O have been evaluated by monitoring acidified acetonitrile solutions of the 2e(-)-reduced clusters by rotating disk electrode voltammetry under anaerobic and aerobic conditions, respectively. Neither of the reduced forms 1b(2e-) nor 2(2e-) reacted under these conditions. In contrast, 1a(2e-) was oxidized via both pathways, consistent with its more negative redox potential, with the rate of oxidation by air-oxygen being significantly faster than that by H+. The present work demonstrated that the crucial step necessary to oxidize reduced catalyst in photocatalytic reactions involving the anions studied may be achieved or accelerated by application of an external potential more positive than the first redox potential of the polyoxometalate anion. Voltammetric analysis revealed that this in situ electrolytic regeneration of the reduced catalyst is an option that leads to a viable photoelectrocatalytic pathway, even when the H+ and O2 pathways are not available. 相似文献
6.
Lennart S. Hultgren 《Applied Scientific Research》1994,53(1-2):99-117
The effects of critical-layer nonlinearity on spatially growing instability waves on shear layers between parallel streams are discussed. In the two-dimensional incompressible case, the flow in the critical layer is governed by a nonequilibrium (unsteady) nonlinear vorticity equation. The initial exponential growth of the instability wave is converted into algebraic growth during the streamwise aging of the critical layer into a quasi-equilibrium state. A uniformly valid composite formula for the instability wave amplitude, accounting for both nonparallel and nonlinear effects, is shown to be in good agreement with available experimental results. Nonlinear effects occur at smaller amplitudes for the three-dimensional and supersonic cases than in the two-dimensional incompressible case. The instability-wave amplitude evolution is then described by one integro-differential equation with a cubic-type nonlinearity, whose inviscid solution always end in a singularity at finite downstream distance.The US Government has the right to retain a nonexclusive royalty-free license in and to any copyright covering this paper. 相似文献
7.
[reaction: see text] Optically active beta-lactams 3 are obtained in excellent yields (up to 93%) and with complete stereoselectivity from Meldrum's acid derivatives 1 and Delta(2)-thiazolines 2. A selective reduction to aldehydes 5 (R = Ar or CH(2)Ar) was then accomplished by using DIBAL-H. This rigid framework, with stereochemistry different than that of penicillin, is designed to be a suitable scaffold for the development of compounds inhibiting pilus formation in uropathogenic Escherichia coli. 相似文献
8.
Substituted bicyclic 2-pyridones, termed pilicides, prevent pilus assembly in uropathogenic Escherichia coli. Based on the bioactive methyl ester protected 2-pyridone 4, further functionalization at C-6 has yielded a set of new compounds, which have been evaluated for their ability to inhibit pilus formation in uropathogenic E. coli. The key intermediate in the synthesis was formylated 2-pyridone 5, which could be obtained via a Vilsmeier reaction. This versatile intermediate was converted into secondary and tertiary amines via reductive amination and could also be converted to other interesting functionalities using simple chemical transformations. 相似文献
9.
Chorell E Pinkner JS Bengtsson C Edvinsson S Cusumano CK Rosenbaum E Johansson LB Hultgren SJ Almqvist F 《Chemistry (Weinheim an der Bergstrasse, Germany)》2012,18(15):4522-4532
Pilicides and curlicides are compounds that block the formation of the virulence factors pili and curli, respectively. To facilitate studies of the interaction between these compounds and the pili and curli assembly systems, fluorescent pilicides and curlicides have been synthesized. This was achieved by using a strategy based on structure-activity knowledge, in which key pilicide and curlicide substituents on the ring-fused dihydrothiazolo 2-pyridone central fragment were replaced by fluorophores. Several of the resulting fluorescent compounds had improved activities as measured in pili- and curli-dependent biofilm assays. We created fluorescent pilicides and curlicides by introducing coumarin and 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (BODIPY) fluorophores at two positions on the peptidomimetic pilicide and curlicide central fragment. Fluorescence images of the uropathogenic Escherichia coli (UPEC) strain UTI89 grown in the presence of these compounds shows that the compounds are strongly associated with the bacteria with a heterogeneous distribution. 相似文献
10.
Allison M Fox Mike Anderson Corinne Reid Tim Smith Dorothy VM Bishop 《BMC neuroscience》2010,11(1):1-15