Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists with greater selectivity over hERG were identified. SAR studies addressing two distinct alternatives for structural modifications leading to improve hERG selectivity are described.
Meyers
Kenneth M
KM
Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA.
Kim
Nicholas
N
Méndez-Andino
José L
JL
Hu
X Eric
XE
Mumin
Rashid N
RN
Klopfenstein
Sean R
SR
Wos
John A
JA
Mitchell
Maria C
MC
Paris
Jennifer L
JL
Ackley
David C
DC
Holbert
Jerry K
JK
Mittelstadt
Scott W
SW
Reizes
Ofer
O
D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D000072237:ERG1 Potassium Channel; D004873:Ergolines / Q000494:pharmacology; D051638:Ether-A-Go-Go Potassium Channels / Q000187:drug effects*; D006801:Humans; D007202:Indicators and Reagents; D008803:Mianserin / Q000494:pharmacology; D009281:Naphthalenes / Q000138:chemical synthesis / Q000494:pharmacology*; D026902:Potassium Channel Blockers / Q000494:pharmacology*; D044405:Receptor, Serotonin, 5-HT2C / Q000187:drug effects; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D012702:Serotonin Antagonists / Q000494:pharmacology; D013329:Structure-Activity Relationship
D001713:Biphenyl Compounds; D000072237:ERG1 Potassium Channel; D004873:Ergolines; D051638:Ether-A-Go-Go Potassium Channels; D007202:Indicators and Reagents; C000606913:KCNH2 protein, human; C103263:MCHR1 protein, human; D009281:Naphthalenes; D026902:Potassium Channel Blockers; D044405:Receptor, Serotonin, 5-HT2C; D017481:Receptors, Somatostatin; D012702:Serotonin Antagonists; C518530:aminomethyl tetrahydronaphthalene biphenyl carboxamide; D008803:Mianserin; C031649:mesulergine