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  • 1
    Electronic Resource
    Electronic Resource
    Synthesis of the bradykinin B1 antagonist [desArg10]HOE 140 on 2-chlorotrityl resin (1996)
    Springer
    International journal of peptide research and therapeutics 2 (1996), S. 319-323 
    Details
    ISSN: 1573-3904
    Keywords: Difficult sequence ; Diketopiperazine ; Solid-phase peptide synthesis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary This paper describes the synthesis of the bradykinin B1 antagonist [desArg10]HOE 140 (d-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-d-Tic-Oic-OH) by the solid-phase method. This synthesis is predicted to be a difficult one because the C-terminal sequence d-Tic-Oic, when linked to the resin, could easily undergo an intramolecular aminolysis, releasing the corresponding diketopiperazine. This reaction is greatly favored by the imino acidic structure of these two residues and by the d-configuration of the second one. When using the Fmoc strategy, the reaction takes place during the Fmoc removal with piperidine. In this case, it has been suggested previously that it is possible to prevent the side reaction by reducing the time of the base treatment. In our hands, this expedient worked correctly for the synthesis of a test tetrapeptide (H-Gly-Pro3-OH), but under the same conditions the synthesis of the target peptide failed completely. In contrast, the use of the very hindered 2-chlorotrityl resin reduced diketopiperazine formation to undetectable levels.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00119994
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  • 2
    Electronic Resource
    Electronic Resource
    Conformational rigidity versus flexibility in a novel peptidic neurokinin A receptor antagonist (1995)
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Peptide Science 1 (1995), S. 236-240 
    Details
    ISSN: 1075-2617
    Keywords: Tachykinins ; NK-2 antagonist ; cyclic peptide ; conformation ; Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Neurokinin A receptor antagonists have been proposed as a new class of drugs for several applications in humans (asthama, intestinal motility, etc.). The rational design, synthesis, structural characterization and biological activity evaluation of a new potent, highly selective, long-lasting, peptide-based receptor antagonist are reported. The structure-activity relationship indicates that the conformational rigidity determines potency, specificity and especially the long life of the molecule in the living body. MEN 10627 is the prototype of a new class of cyclic, peptide-based, neurokinin A receptor antagonists and it is a suitable candidate for clinical testing in humans.
    Additional Material: 3 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/psc.310010404
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