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81.
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
82.
We prove that for every fixed k and ? ≥ 5 and for sufficiently large n, every edge coloring of the hypercube Qn with k colors contains a monochromatic cycle of length 2 ?. This answers an open question of Chung. Our techniques provide also a characterization of all subgraphs H of the hypercube which are Ramsey, that is, have the property that for every k, any k‐edge coloring of a sufficiently large Qn contains a monochromatic copy of H. © 2006 Wiley Periodicals, Inc. J Graph Theory 53: 196–208, 2006 相似文献
83.
Jeannette Van Iseghem 《Numerical Algorithms》2002,29(1-3):267-279
A method for solving a linear system is defined. It is a Lanczos-type method, but it uses formal vector orthogonality instead of scalar orthogonality. Moreover, the dimension of vector orthogonality may vary which gives a large freedom in leading the algorithm, and controlling the numerical problems. The ideas of truncated and restarted methods are revisited. The obtained residuals are exactly orthogonal to a space of increasing dimension. Some experiments are done, the problem of finding automaticaly good directions of projection remains partly open. 相似文献
84.
Remco van der Hofstad Gerard Hooghiemstra Piet Van Mieghem 《Random Structures and Algorithms》2002,20(4):519-539
In this paper we study the covariance structure of the number of nodes k and l steps away from the root in random recursive trees. We give an analytic expression valid for all k, l and tree sizes N. The fraction of nodes k steps away from the root is a random probability distribution in k. The expression for the covariances allows us to show that the total variation distance between this (random) probability distribution and its mean converges in probability to zero. © 2002 Wiley Periodicals, Inc. Random Struct. Alg., 20: 519–539, 2002 相似文献
85.
We prove that a for a mapping f of finite distortion , the -Hausdorff measure of any point preimage is zero provided is integrable, with , and the multiplicity function of f is essentially bounded. As a consequence for we obtain that the mapping is then open and discrete.
Received: 18 June 2001 / Revised version: 31 January 2002 / Published online: 27 June 2002 相似文献
86.
Jan E. Åman Ingemar Bengtsson Narit Pidokrajt 《General Relativity and Gravitation》2006,38(8):1305-1315
The Hessian of either the entropy or the energy function can be regarded as a metric on a Gibbs surface. For two parameter families of asymptotically flat black holes in arbitrary dimension one or the other of these metrics are flat, and the state space is a flat wedge. The mathematical reason for this is traced back to the scale invariance of the Einstein–Maxwell equations. The picture of state space that we obtain makes some properties such as the occurence of divergent specific heats transparent.Supported by VR. 相似文献
87.
Ngo Quang Huy Trinh Thi Bich Nguyen Van Suc 《Journal of Radioanalytical and Nuclear Chemistry》2006,269(1):129-133
Summary The paper presents a procedure to prepare soil samples for U and Th isotope measurement by alpha-spectrometry after coprecipitation
with LaF3. In this procedure the reduction of U(VI) to U(IV) was performed by Zn metal in 4M HCl solution. The recoveries of chemical
separation equal to eU-chemistry = 78±4% for uranium and eTh-chemistry = 82±4% for thorium. Canberra alpha-spectrometer was used with PIPS detectors of A-1200-37-AM Model of 1200 mm2 active area. The counting efficiency of the measuring system equals to ecounting = 18% and the total efficiencies were eU = ecounting .eU-chemistry = 14.0±0.7% for uranium and eTh = ecounting .eTh-chemistry = 14.7±0.7% for thorium. The recoveries of chemical separation were rather high (about 80%), that leads to the use of a small
weight of soil sample (about 0.5 g). The efficiencies were also stable, that allows analyzing the soil sample without using
radiotracers. They are advantages of the sample preparation procedure of this work. 相似文献
88.
Cornelis Van de Panne 《The Journal of the Operational Research Society》1992,43(12):1159-1171
The paper deals with the appropriate form of interaction between two refineries with different demand patterns. This problem can be formulated as finding a decentralized solution of linear programming problems linked by buying and selling activities. The complete problem is first solved for central values of product demands and costs and revenues. The structure of the basis then determines the organization of the interaction in terms of which unit sets quantities and which prices, or whether centralized decisions should be made. If, for expected values of product demand and costs, the structure of the basis is the same then the related organization of trading can be used for day-to-day transactions. For a well-known oil refinery model it is found that, for fairly large demand variations, decentralized interaction is effective, but that the structure of the basis changes easily with crude price variations, and that simulations did not converge for these variations. 相似文献
89.
Michal Johanis Jan Rychtá r 《Proceedings of the American Mathematical Society》2007,135(5):1511-1514
It is shown that every separable Banach space admits an equivalent norm that is uniformly Gâteaux smooth and yet lacks asymptotic normal structure.
90.
6-Thia-l-aza-5λ5-phosphabicyclo[3.2.0]hept-3-enes and Isothiocyanatophosphine-sulfides from (Methylidenamino)phosphines, Carbon Disulfide, and Acetylene- or Ethylene Derivatives (Methylidenamino)phosphines react with carbon disulfide to 1,3,2-thiazaphosphete derivatives 2 . Acetylenedicarboxylates give with 2 6-thia-l-aza-5λ5-phosphabicyclo[3.2.0]hept-3-enes 4a , b , and acrylates yield isothio-cyanatophosphin-sulfides 5a – c . The structures of 4a and 5a are proven by an X-ray diffraction analysis. 相似文献