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Modular synthesis of non-peptidic bivalent NPY Y(1) receptor antagonists

Weiss, Stefan, Keller, Max, Bernhardt, Günther, Buschauer, Armin and König, Burkhard (2008) Modular synthesis of non-peptidic bivalent NPY Y(1) receptor antagonists. Bioorganic & Medicinal Chemistry 16 (22), pp. 9858-9866.

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According to a 'bivalent ligand approach' to increase the affinity of the potent argininamide-type NPY Y(1) receptor antagonist BIBP-3226, dimeric ligands were synthesized in which two molecules of the parent compound were linked by different spacers via N(G)-acylation at the guanidino groups. A synthetic route for the preparation of the title compounds was developed, which includes a ...


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Item type:Article
Date:13 September 2008
Institutions:Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
18851917PubMed ID
Related URLs:
http://www.sciencedirect.com/science/MiamiMultiMediaURL/B6TF8-4TF7C77-7/B6TF8-4TF7C77-7-1/5220/0560afe0f3d32f50f51c42fee5e230ae/mmc1.pdfSupplementary Material
Keywords:bivalent ligands; neuropeptide Y; NPY; Y1 receptor antagonist; argininamides; BIBP 3226; guanidinium compounds; Huisgen reaction; cycloaddition
Dewey Decimal Classification:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:4680
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