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N(G)-Acyl-argininamides as NPY Y (1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity

Weiss, Stefan and Keller, Max and Bernhardt, G. and Buschauer, Armin and König, Burkhard (2010) N(G)-Acyl-argininamides as NPY Y (1) receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity. Bioorganic & Medicinal Chemistry (18), pp. 6292-6304.

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Abstract

N(G)-Acylated argininamides, covering a broad range of lipophilicity (calculated logD values: -1.8-12.5), were synthesized and investigated for NPY Y(1) receptor (Y(1)R) antagonism, Y(1)R affinity and stability in buffer (N(G)-deacylation, yielding BIBP 3226). Broad structural variation of substituents was tolerated. The K(i) (binding) and K(b) values (Y(1)R antagonism) varied from low nM to ...

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Item Type:Article
Date:2010
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:
ValueType
20688523PubMed ID
10.1016/j.bmc.2010.07.028 DOI
Keywords:Acyl guanidines, NPY, BIBP 3226, GPCR
Subjects:500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Regina Hoheisel
Deposited On:20 Oct 2010 08:59
Last Modified:15 Dec 2010 08:17
Item ID:16340
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