N-acylated alpha-(3-pyridylmethyl)-beta-aminotetralin antagoinists of the human neuropeptide Y Y5 receptor.
Alpha-(3-Pyridylmethyl)-beta-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.
McNally
J J
JJ
Drug Discovery, The R. W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA.
Youngman
M A
MA
Lovenberg
T W
TW
Nepomuceno
D
D
Wilson
S
S
Dax
S L
SL
D015081:2-Naphthylamine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D000215:Acylation; D006801:Humans; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*
D011725:Pyridines; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor; D015081:2-Naphthylamine