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Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226
I Aiglstorfer1, I Hendrich, C Moser
1Institute of Pharmacy, University of Regensburg, Germany.
Bioorganic & Medicinal Chemistry Letters
|July 29, 2000
Abstract:
Analogues of BIBP 3226, (R)-N(alpha)-diphenylacetyl-N-(4-hydroxybenzyl)argininamide, were synthesized and investigated for Y1 antagonism (Ca2+-assay, HEL cells) and binding on Y1, Y2 and Y5 receptors. Replacing the benzylamino by a tetrahydrobenzazepinyl group preserves most of the Y1 activity. Combination with a N(G)-phenylpropyl arginine and a N(alpha)-p-biphenylylacetyl moiety shifted the NPY receptor selectivity towards Y5.