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Peptidosulfonamides are an emerging group of peptidomimetics with a variety of applications in medicinal chemistry. We present a novel approach to the synthesis of peptidosulfonamides, and apply it to a series of new potential inhibitors of the bacterial peptidoglycan biosynthesis enzymes MurD and MurE. The synthesis was conducted via N-phthalimido β-aminoethanesulfonyl chlorides, which are new building blocks for the synthesis of peptidosulfonamides. In the most crucial step, sulfonic acids or their sodium salts were converted into the corresponding sulfonyl chlorides using an excess of either SOCl2 or SOCl2/DMF, and then coupled to the C-protected amino acid. None of the compounds significantly inhibited MurD, however, some inhibited MurE; one had an IC50 below 200 μM, which constitutes a promising starting point for further development. Molecular modelling simulations were performed on two analogues to investigate the absence of inhibitory activity of the sulfonamide compounds on MurD.  相似文献   
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?engül Dilem Yard?mc? 《Tetrahedron》2006,62(46):10633-10638
The photooxygenation of the 1-methyl-, 2,3-dimethyl-, and 1,4-dimethylcyclohexa-1,4-dienes, which are readily available through Birch reduction, yielded the corresponding ene-products. The formed endocyclic dienes were trapped by the addition of singlet oxygen to give the corresponding bicyclic endoperoxy hydroperoxides. In the case of 1-methylcyclohexa-1,4-diene and 1,4-dimethylcyclohexa-1,4,-diene, the cis-effect determined the product distribution. Photooxygenation of 2,3-dimethylcyclohexa-1,4-dienes gave mainly exocyclic olefin, which was attributed to the lowered rotational barrier of the methyl group and increased reactivity of the methyl groups.  相似文献   
65.
Cr-doped mullites were prepared from single-phase precursors containing up to 9.60 wt% Cr2O3 using a sol-gel technique followed by thermal treatment. Particle induced X-ray emission spectroscopy and X-ray powder diffraction were used to characterize the samples. Mullites were orthorhombic, space group Pbam. Cr doping caused the increase of unit-cell parameters. Strongest expansion was noticed along c-axis followed by a and bc/c=0.089, Δa/a=0.061, Δb/b=0.045% per mole Cr2O3). A second phase, namely θ-(Al,Cr)2O3, was revealed by XRD in the sample containing 9.60 wt% Cr2O3. The structure of mullites was refined by the Rietveld method, location of Cr3+ was performed by the EPR spectroscopy. At low chromium doping level (Cr2O3 content less than ∼5 wt%) Cr3+ ions were substituted for Al3+ in the AlO6 octahedra of the mullite structure (M1 site). For higher doping level, Cr3+ ions were additionally substituted for Al3+ in the AlO6 octahedra of the second phase [θ-(Al,Cr)2O3 at 1400 °C, or α-(Al,Cr)2O3 at 1600 °C] which segregated in the system. Substitution of Cr3+ for Al3+ on M1 site in the mullite structure resulted in increase of average distances in (M1)O6 octahedron and decrease of average distances in T*O4 tetrahedron, while average distances in TO4 tetrahedron stayed almost constant.  相似文献   
66.
Holography is a promising technique for power combining applications in the frequency range of short millimeter and submillimeter waves. In this paper, quasi-optical holographic power combining circuits are investigated. An equivalent network is utilized which rigorously models horn arrays and biperiodic dielectric structures in order to design computer-generated holograms. We apply the network model to a 5-element quasi-optical power combiner and demonstrate its capability. The hologram is designed for 150 GHz and has an efficiency of 92.5 % with a 90 % bandwidth of 5.3 %. With the aid of a broadband waveguide power divider and a vector field measurement system, the circuit is analyzed.  相似文献   
67.
A general method to convert single-stranded, chemically synthesized oligonucleotides into cloned duplexes is described. Oligonucleotides supplied with 3'-terminal extensions that are complementary to 3'-protruding ends obtained by certain restriction enzymes can be cloned either directly or with the help of an adapter molecule into double-stranded vectors. Two methods have also been developed for consecutive cloning applications. According to these methods, the synthetic oligonucleotides (and their enzymatically prepared complementary strands) are joined, one after the other, inside a cloning vector, each joining requiring one cloning step. Synthetic genes are thus built up from oligonucleotides corresponding to only one strand of the DNA. The sequential assembly of the cloned duplex takes place in the 5' to 3' direction. Each oligonucleotide is supplied with a four-nucleotide-long 3'-terminal extension, but this sequence is eliminated when the joining takes place, leaving no limiting sequence between the oligonucleotides. The two consecutive cloning methods, the adapter and the polycloning site methods, are illustrated by the assembly of short artificial genes.  相似文献   
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We use a newly introduced concept of neocompactness to study problems from metric fixed point theory. In particular, we give a sufficient condition for a superreflexive Banach space X to have the fixed point property and obtain shorter proofs of some well-known results in that theory.  相似文献   
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