Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists.
A series of piperazinephenethylamines were synthesized to study the contribution of a basic amine to binding affinity at the melanocortin-4 receptor. Several potent compounds from this series possessed subnanomolar K(i) values in a competition binding assay.
Tran
Joe A
JA
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Arellano
Melissa
M
Fleck
Beth A
BA
Pontillo
Joseph
J
Marinkovic
Dragan
D
Tucci
Fabio C
FC
Wen
Jenny
J
Saunders
John
J
Chen
Chen
C
D000818:Animals; D001596:Benzylamines / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007700:Kinetics; D010627:Phenethylamines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D001596:Benzylamines; D010627:Phenethylamines; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4