Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor.
Synthesis and structure-activity relationship studies of a series of cyclohexylpiperazines bearing an amide side chain as ligands of the MC4 receptor are discussed. Compounds such as 11i from this series are potent agonists (EC(50)=33nM, IA=96%).
Pontillo
Joseph
J
Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Tran
Joe A
JA
White
Nicole S
NS
Arellano
Melissa
M
Fleck
Beth A
BA
Marinkovic
Dragan
D
Tucci
Fabio C
FC
Saunders
John
J
Foster
Alan C
AC
Chen
Chen
C
D044482:Benzeneacetamides / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists*; D013329:Structure-Activity Relationship
D044482:Benzeneacetamides; D008024:Ligands; C470072:MC4R protein, human; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4