Propionylpiperazines as human melanocortin-4 receptor ligands.
A series of alpha-benzylpropionylpiperazines were synthesized and tested as antagonists of the melanocortin-4 receptor. In addition to its high potency and selectivity, R-11a had desirable pharmacokinetic properties including high brain penetration in mice.
Chen
Caroline W
CW
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Tran
Joe A
JA
Jiang
Wanlong
W
Tucci
Fabio C
FC
Arellano
Melissa
M
Wen
Jenny
J
Fleck
Beth A
BA
Marinkovic
Dragan
D
White
Nicole S
NS
Pontillo
Joseph
J
Saunders
John
J
Madan
Ajay
A
Foster
Alan C
AC
Chen
Chen
C
D000577:Amides / Q000737:chemistry; D000818:Animals; D006801:Humans; D008024:Ligands; D051379:Mice; D015394:Molecular Structure; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000577:Amides; D008024:Ligands; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4; D000077489:Piperazine