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1.
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
2.
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
3.
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
4.
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
5.
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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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
9.
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
10.
Stratos Ioannidis Oualid Jouini Angelos A. Economopoulos Vassilis S. Kouikoglou 《Annals of Operations Research》2013,209(1):115-138
We consider problems of inventory and admission control for make-to-stock production systems with perishable inventory and impatient customers. Customers may balk upon arrival (refuse to place orders) and renege while waiting (withdraw delayed orders) during stockouts. Item lifetimes and customer patience times are random variables with general distributions. Processing, setup, and customer inter-arrival times are however assumed to be exponential random variables. In particular, the paper studies two models. In the first model, the system suspends its production when its stock reaches a safety level and can resume later without incurring any setup delay or cost. In the second model, the system incurs setup delays and setup costs; during stockouts, all arriving customers are informed about anticipated delays and either balk or place their orders but cannot withdraw them later. Using results from the queueing literature, we derive expressions for the system steady-state probabilities and performance measures, such as profit from sales and costs of inventory, setups, and delays in filling customer orders. We use these expressions to find optimal inventory and admission policies, and investigate the impact of product lifetimes and customer patience times on system performance. 相似文献