PMID: 9431025Feb 12, 1998Paper

Synthesis and neuropeptide Y Y1 receptor antagonistic activity of N,N-disubstituted omega-guanidino- and omega-aminoalkanoic acid amides

Archiv der Pharmazie
M MüllerArmin Buschauer

Abstract

Potent arpromidine-type histamine H2 receptor agonists such as BU-E-76 (He 90481) were among the first non-peptides reported to display weak neuropeptide Y (NPY) Y1 receptor antagonist activity. In search of new chemical leads for the development of more potent NPY antagonists, a series of N,N-disubstituted omega-guanidino and omega-aminoalkanoic acid amides were synthesized on the basis of structure-activity relationships and molecular modeling studies of arpromidine and related imidazolylpropylguanidines. In one group of compounds the imidazole ring was retained whereas in the second group it was replaced with a phenol group representing a putative mimic of Tyr36 in NPY. Although the substitution patterns have not yet been optimized, the title compounds are NPY Y1 antagonists in human erythroleukemia (HEL) cells (Ca2+ assay) achieving pKB values in the range of 6.3-6.6. For representative new substances tested in the isolated guinea pig right atrium histamine H2 receptor agonism could not be found. In the N-(diphenylalkyl)amide series, compounds with a trimethylene chain were more active Y1 antagonists than the ethylene homologs. Concerning the spacer in the omega-amino or omega-guanidinoalkanoyl portion, the best activity wa...Continue Reading

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Citations

May 3, 2016·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·S LiebJ Wegener
Aug 30, 2005·Current Opinion in Chemical Biology·Richard J Middleton, Barrie Kellam
Sep 22, 2007·Journal of Receptor and Signal Transduction Research·Ralf ZiemekArmin Buschauer
Sep 19, 2007·Chembiochem : a European Journal of Chemical Biology·Erich SchneiderArmin Buschauer
Aug 5, 2006·Chembiochem : a European Journal of Chemical Biology·Erich SchneiderArmin Buschauer
Apr 12, 2000·Journal of Peptide Science : an Official Publication of the European Peptide Society·C Cabrele, A G Beck-Sickinger
Jun 15, 2019·International Journal of Molecular Sciences·Ziguo SongChao Sun

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