Aryl piperazine melanocortin MC4 receptor agonists.
Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC(50)=24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds using in vitro cAMP functional assays in cells transfected with the MC4 or other melancortin receptors.
Dyck
Brian
B
Department of Medicinal Chemistry, Neurocrine Biosciences Inc., 10555 Science Center Drive, San Diego, CA 92121, USA.
Parker
Jessica
J
Phillips
Teresa
T
Carter
Lee
L
Murphy
Brian
B
Summers
Robin
R
Hermann
Julia
J
Baker
Tracy
T
Cismowski
Mary
M
Saunders
John
J
Goodfellow
Val
V
D002460:Cell Line; D000242:Cyclic AMP / Q000378:metabolism / Q000502:physiology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D006860:Hydrogen Bonding; D007202:Indicators and Reagents; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000235:genetics; D013329:Structure-Activity Relationship; D014162:Transfection
D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4; D000242:Cyclic AMP