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Introduction mimetics

Example 14 an efficient strategy has been described by Koganty and his associates for the synthesis of compound which is a novel lipid A mimetic [42] The multi-step synthesis is exemplified from the introduction of the phosphate moiety onwards. [Pg.108]

Heparinoid polysaccharides such as heparan sul te and heparin are able to interact with numerous proteins and influence vital biological processes. Heparinoid mimetics were prepared to reduce the structural complexity of heparinoids and to obtain selectivities. This artide summarizes the development of heparinoid mimetics of different classes including representative syntheses and biological activities. Largely simplified compounds with regard to structure and synthetic access are described which maintain or exceed the activity of heparinoid polysaccharides. One of the recipes to increase binding or modify pharmacokinetic parameters was the introduction of hydrophobic groups. [Pg.215]

Creative interplay between colloid and polymer chemistries has increasingly contributed to the development of membrane-mimetic systems and advanced materials. On the one hand, the employment of polymer methodologies and/or the addition of polymers have favorably altered the properties of colloidal systems. On the other hand, the introduction of surfactants and surfactant assemblies prior, during, or subsequent to polymerization has resulted in distinctly different polymers. [Pg.88]

The idealized mimetic 34 (Scheme 14) was designed to incorporate the ability to introduce functionality at each of the positions R1, R2, R3, and R4, and both an amino and carboxy terminus for coupling to peptide chains. The stereospecific and regiospecific synthesis of a molecule which contains six nonadjacent asymmetric centers proved to be a difficult task. Model studies for the synthesis were performed. 88 The salient feature of this synthesis was an acylimminium cyclization 89 coupled with a tin hydride induced radical cyclization (Scheme 18). 90 Unfortunately, we were not able to readily relate the introduction of the... [Pg.704]

F ure 3.28. Peptidomimetics that have been designed based on iterative introduction of constraints into parent peptide and hypotheses concerning receptor-bound conformation. Enkephalin mimetic (388), RGD platelet GPIIb/IIIa receptor antagonists (384,385), thyrohberin [TRH (387)], and somatostatin (383,389).For an overview of recent approaches to peptidomimetic design, see the review by Bursavich and Rich (382). [Pg.129]

Figure 22. (a) A fragment of the photosynthetic reaetion center with the three eomponents Speeial Pair (SP), Accessory Baeteriochlorophyll (BCh), and Bacteriopheophytin (BPh). Photoindueed electron transfer from SP to BPh takes place at a i lobal rate of (3 ps). (b) Prineiple of the modular mimetic approach. D and A are the donor and aeceptor porphyrins, respectively. M is an eleetron transfer mediator whose introduction between D and A can be realized via coordination of a metal center (solid circle) which will also bind the chelating part of the bisporphyrin spacer. [Pg.2281]

Peptides containing amino acids in which the a-proton has been replaced by a methyl group or other alkyl group (a,a-dialkyl amino acids) serve as the simplest example of helix mimetics. The severe restrictions of (p,v / space by an a-methyl amino acid to limit backbone conformations only to values associated with both a- and 310-heli-ces was discovered independently by Marshall and Bosshard (90) and by Burgess and Leach (171). These early predictions from molecular modeling have been confirmed by multiple studies, both computationally (172-175) and experimentally (176-183) in the subsequent 35 years. Numerous examples of the introduction of a-methyl amino acids into biologically... [Pg.143]

With the introduction of incretin mimetics, the first new class of diabetes agents in nearly 20 years is now available. Incretins improve glucose control but also have the potential to improve insulin resistance and to restore p-cell function. [Pg.1272]

Introduction of constraints by secondary structure mimetics ( turns, loops, p-sheets and a-helix-mimetics)... [Pg.188]

A comprehensive review (260 refs.) on the synthesis of carbohydrates from noncarbohydrate sources covers the use of benzene-derived diols and products of Sharpless asymmetric oxidation as starting materials, Dodoni s thiazole and Vogel s naked sugar approaches, as well as the application of enzyme-catalysed aldol condensations. The preparation of monosaccharides by enzyme-catalysed aldol condensations is also discussed in a review on recent advances in the chemoenzymic synthesis of carbohydrates and carbohydrate mimetics, in parts of reviews on the formation of carbon-carbon bonds by enzymic asymmetric synthesis and on carbohydrate-mediated biochemical recognition processes as potential targets for drug development, as well as in connection with the introduction of three Aldol Reaction Kits that provide dihydroxyacetone phosphate-dependent aldolases (27 refs.). A further review deals with the synthesis of carbohydrates by application of the nitrile oxide 1,3-dipolar cycloaddition (13 refs.). ... [Pg.2]

While a number of organisms have been investigated as potential hosts for the expression of elastin-mimetic polypeptide sequences, bacterial strains of E. coli remain the preferred cellular host for these experiments. Escherichia coli strains have a number of advantages for these applications, which include the availability of highly effective expression plasmids, the potential for introduction of genomic modifications, a well-characterized physiological response, simple... [Pg.91]


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See also in sourсe #XX -- [ Pg.2 , Pg.3 ]




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