N-Acylated α-(3-pyridylmethyl)-β-aminotetralin antagonists of the human neuropeptide Y Y5 receptor

α-(3-Pyridylmethyl)-β-aminotetralins were acylated with amino-piperidinyl and-pyrrolidinyl acetic acids, and with (aminomethyl)cyclohexanecarboxylic acid. Reaction with acyl chlorides, chloroformates, and isocyanates gave amides 8e, carbamates 9, and ureas 10, which bound to the Y5 receptor with nan...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 10; no. 15; pp. 1641 - 1643
Main Authors McNally, James J, Youngman, Mark A, Lovenberg, Timothy W, Nepomuceno, Diane, Wilson, Sandy, Dax, Scott L
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 07.08.2000
Elsevier
Subjects
Biological and medical sciences
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Human
Neuropeptide Y
Nitrogen heterocycle
In vitro
Naphthalene derivatives
Pyridine derivatives
Structure activity relation
Benzimidazole derivatives
Piperidine derivatives
Phenols
Peptidergic receptor
Carboxamide
Ureas
Aromatic compound
Antagonist
Chemical synthesis
Online AccessGet full text

Cover

More Information
Summary:α-(3-Pyridylmethyl)-β-aminotetralins were acylated with amino-piperidinyl and-pyrrolidinyl acetic acids, and with (aminomethyl)cyclohexanecarboxylic acid. Reaction with acyl chlorides, chloroformates, and isocyanates gave amides 8e, carbamates 9, and ureas 10, which bound to the Y5 receptor with nanomolar affinity. Congeners 11a and 11d containing a terminal benzimidazolone group were shown to be functional Y5 antagonists.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00311-5