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排序方式: 共有71条查询结果,搜索用时 15 毫秒
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Nicolaou KC Cho SY Hughes R Winssinger N Smethurst C Labischinski H Endermann R 《Chemistry (Weinheim an der Bergstrasse, Germany)》2001,7(17):3798-3823
Vancomycin, the prototypical member of the glycopeptide family of antibiotics, is a clinically used antibiotic employed against a variety of drug-resistant bacterial strains including methicillin-resistant Staphylococcus aureus (MRSA). The recent emergence of vancomycin resistance, viewed as a growing threat to public health, prompted us to initiate a program aimed at restoring the potency of this important antibiotic through chemical manipulation of the vancomycin structure. Herein, we describe the development of synthetic technology based on the design of a novel selenium safety catch linker, application of this technology to a solid-phase semisynthesis of vancomycin, and the solid- and solution-phase synthesis of vancomycin libraries. Biological evaluation of these compound libraries led to the identification of a number of in vitro highly potent antibacterial agents effective against vancomycin-resistant bacteria. In addition to aiding these investigations, the solid-phase chemistry described herein is expected to enhance the power of combinatorial chemistry and facilitate chemical biology and medicinal chemistry studies. 相似文献
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Alexander Chernega Dirk. L. Elend Christian A.P. Smethurst Paul M. Roberts Andrew D. Smith G. Darren Smyth 《Tetrahedron》2007,63(30):7036-7046
A three-step protocol for the asymmetric synthesis of a range of β-substituted Baylis-Hillman products has been developed. This procedure involves the diastereoselective conjugate addition of lithium (R)-N-methyl-N-(α-methylbenzyl)amide to an α,β-unsaturated ester to generate an N-protected β-amino ester in high de. Subsequent asymmetric aldol reaction via deprotonation with LDA, transmetallation with B(OMe)3 and addition of an aldehyde gives a range of syn-aldol products in moderate to high de. Purification of the syn-aldol products to homogeneity followed by tandem N-oxidation and Cope elimination gives the desired β-substituted Baylis-Hillman products in good yield and high de and ee. 相似文献
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Suwannee Junyapoon Keith D. Bartle Andrew B. Ross Michael Cooke Brian F. Smethurst 《International journal of environmental analytical chemistry》2013,93(4):337-348
Abstract Trace volatile compounds emitted from both domestic and industrial landfills have been identified by programmed temperature vaporization injection (PTV) coupled to gas chromatography with detection by ion-trap mass spectrometry (GC-ITD/MS). The PTV injection system has been developed using a combination of two six-port valves to achieve problems of interference in GC-MS while loading sample. A large volume of landfill gas was re-concentrated onto a sorbent trap, then rapidly liberated into the GC-ITD/MS system by programmed thermal desorption. Using this method, trace volatile compounds in gases from both domestic and industrial landfills such as aromatic hydrocarbons, terpenes, chlorinated hydrocarbons, and sulfur compounds can be identified and quantified. 相似文献
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Liondas CA; Chrissoulidis DP 《The Quarterly Journal of Mechanics and Applied Mathematics》2007,60(3):275-287
This paper is intended to clarify a misunderstanding concerningthe source singularity of the electric Green's tensor for aperfectly conducting semi-infinite cone of circular cross-section.Tai's series expansion of the Green's tensor is known to lacka singular term at the source region. Jones has reconstructedthe solution to this problem and has pointed out the differencebetween his result and that of Tai. The aim of our paper isto demonstrate that, although Jones's closed-form solution iscorrect, there is a mistake in his comparison with Tai's seriessolution. We conclude that one of the two additional singularterms that Jones claims as missing from Tai's formula must beomitted. Besides, we compare Jones's closed-form solution withSmyshlyaev's solution to the very same problem. We concludethat the magnetic field expressions given by Jones and Smyshlyaevcoincide, but a singular term is missing from Smyshlyaev's expressionfor the electric field. 相似文献
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Goodman TNT; Micchelli CA; Rodriguez G; Seatzu S 《IMA Journal of Numerical Analysis》1998,18(3):331-354
It is shown that, under certain conditions, orthonormalizingthe positive integer shifts of an exponentially decaying functionon the half line by the Gram-Schmidt process leads to a limitingprofile given by orthonormalizing all their integer shifts onthe whole line. These results derive from properties of Choleskyfactorization of bi-infinite and semi-infinite matrices. Anexample is provided by the negative exponential function andconjectures are given, supported by numerical evidence, forthe Gaussian and Lorentz function. 相似文献
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从烟草(品种革新一号)单倍体花粉植株的叶和茎产生的愈伤组织,结合悬浮培养,获得的细胞分离出原生质体。在液体培养基中静置培养,12小时后原生质体开始变为卵圆形,细胞壁明显可见,24小时后完成第一次细胞分裂。以后继续分裂形成浅黄色的愈伤组织,在培养四星期后可达1毫米大小,再放到转床上进行旋转培养18天左右,愈伤组织可达3—4毫米大小。当转移到分化培养基后,分别分化出苗及根,长成完整的植株。 原生质体再生细胞的分裂与分化,不仅受不同器官来源的愈伤组织及其年龄的影响;还受分化培养基的基本成份及所用细胞分裂素的类型等的影响。 相似文献
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本文利用中心流面法的概念,指出叶轮机械的设计白变数在内、外环壁面上应有附加的限制条件,并导得其具体简明方程。同时,还定性地分析了S1流面的翘曲情况。 相似文献