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van Hooft PA El Oualid F Overkleeft HS van der Marel GA van Boom JH Leeuwenburgh MA 《Organic & biomolecular chemistry》2004,2(9):1395-1403
The scope of a stereoselective three-step approach for the synthesis of sugar derived spiroketals is presented. The methodology consists of Grignard addition of vinyl- or allylmagnesium bromide to a carbohydrate lactone, followed by K-10 clay mediated glycosidation with a terminal alkenol and subsequent ring-closing metathesis of the resulting diene. The generality of this procedure is demonstrated by the synthesis of various pyranose- and furanose-derived spiroketals, as well as more advanced tricyclic spiroketal derivatives. It is shown that functionalisation of the double bond in the resulting spiroketals leads to fused polycyclic ethers. 相似文献
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Radia Bouasla Hadjira Berredjem Malika Berredjem Malika Ibrahim‐Oualid Assia Allaoui Marc Lecouvey Nour‐Eddine Aouf 《Journal of heterocyclic chemistry》2013,50(6):1328-1332
A new series of chiral 5‐substituted bis‐oxazolidinones containing an acylsulfonamide moiety has been synthesized starting from chlorosulfonyl isocyanate, (l )‐ethyl lactate, and oxazolidin‐2‐ones. All the reactions were conducted at ambient temperature, and the N‐acylsulfonamide bis‐oxazolidin‐2‐ones were obtained with high yields within 2 h. Some of the newly synthesized compounds were evaluated in vitro against the virulent strain RH of Toxoplasma gondii and the human lymphocytes, and showed promising results. 相似文献
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El Oualid F van den Elst H Leroy IM Pieterman E Cohen LH Burm BE Overkleeft HS van der Marel GA Overhand M 《Journal of combinatorial chemistry》2005,7(5):703-713
A combinatorial synthesis of oligopeptide analogues and their evaluation as protein:geranylgeranyl transferase inhibitors is presented. The combinatorial strategy is based on the random mutation, in each new generation, of one of any of the four amino acid building blocks of which the most effective compounds of the previous generation are assembled. In this way, a progressive improvement of the average inhibitory activity was observed until the fifth generation. The most active inhibitors were found to inhibit PGGT-1 in the low micromolar range (IC(50): 3.8-8.1 microM). 相似文献
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Grotenbreg GM Kronemeijer M Timmer MS El Oualid F van Well RM Verdoes M Spalburg E van Hooft PA de Neeling AJ Noort D van Boom JH van der Marel GA Overkleeft HS Overhand M 《The Journal of organic chemistry》2004,69(23):7851-7859
A practical gram-scale and high-yielding synthesis of the antimicrobial peptide gramicidin S is presented. An Fmoc-based solid-phase peptide synthesis protocol is employed for the generation of the linear decapeptide precursor, which is cyclized in solution to afford the target compound. The versatility of our method is demonstrated by the construction of eight gramicidin S analogues (15a-h) having nonproteinogenic sugar amino acid residues (4-7) incorporated in the turn regions. 相似文献
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Raunkjaer M El Oualid F van der Marel GA Overkleeft HS Overhand M 《Organic letters》2004,6(18):3167-3170
[reaction: see text] Novel highly functionalized dipeptide isosters are synthesized via a diastereoselective alkyl/arylation protocol of a glucose-derived (R)-tert-butanesulfinylimine. One of these novel sugar amino acid derivatives, a D-Ala-Ser/Thr isostere, was applied in a peptide synthesis protocol to afford a cyclic tetramer. 相似文献
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We consider ordinary and conditional first passage times in a general birth–death process. Under existence conditions, we
derive closed-form expressions for the kth order moment of the defined random variables, k ≥ 1. We also give an explicit condition for a birth–death process to be ergodic degree 3. Based on the obtained results,
we analyze some applications for Markovian queueing systems. In particular, we compute for some non-standard Markovian queues,
the moments of the busy period duration, the busy cycle duration, and the state-dependent waiting time in queue.
相似文献
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Current transport mechanism in Schottky diode containing InAs quantum dots (QDs) is investigated using temperature-varying current-voltage characteristics. We found that the tunnelling emission has obvious effects on the I-V characteristics. The I-V-T measurements revealed clear effects of QDs on the overall current flow. Field emission (FE, pure tunnelling effect) was observed at low temperature and low voltages bias region. The zero-bias barrier height decreases and the ideality factor increases with decreasing temperature, and the ideality factor was found to follow the T0-effect. When the reverse bias is varied, the ideality factors of Schottky barriers exhibit oscillations due to the tunnelling of electrons through discrete levels in quantum dots. The traps distributed within InAlAs layer can also act as a transition step for reverse bias defect-assisted tunnelling current which can phenomenologically explain the decrease of the effective barrier height with measurement temperature. 相似文献
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Clair S Ourdjini O Abel M Porte L 《Chemical communications (Cambridge, England)》2011,47(28):8028-8030
Control on the formation of a two-dimensional polymer could be achieved in two different ways. Manipulation with the tip of a scanning tunneling microscope allowed for assigning the localization of the polymerization reaction. Additionally, electron irradiation could accelerate greatly the reaction kinetics. 相似文献