Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.
The synthesis and biological testing of novel classes of potent melanin-concentrating hormone (MCH-R1) antagonists based on pyrazolopiperazinone and pyrrolopiperazinone scaffolds are described.
Meyers
Kenneth M
KM
Procter and Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA.
Méndez-Andino
José
J
Colson
Anny-Odile
AO
Hu
X Eric
XE
Wos
John A
JA
Mitchell
Maria C
MC
Hodge
Karen
K
Howard
Jeremy
J
Paris
Jennifer L
JL
Dowty
Martin E
ME
Obringer
Cindy M
CM
Reizes
Ofer
O
D018938:Caco-2 Cells; D006801:Humans; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D044405:Receptor, Serotonin, 5-HT2C / Q000187:drug effects; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*
D007202:Indicators and Reagents; C103263:MCHR1 protein, human; D010879:Piperazines; D011720:Pyrazoles; D011758:Pyrroles; D044405:Receptor, Serotonin, 5-HT2C; D017481:Receptors, Somatostatin; C518524:pyrazolopiperazinone; C518525:pyrrolopiperazinone