title: Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists.
abstract: A series of novel 5,5-diphenylimidazolones was synthesized and evaluated for activity against the human neuropeptide Y5 receptor. The 3-pyridyl analog 46 demonstrated an IC(50) of 8.3 nM with a favorable pharmacokinetic profile in rats, but was ineffective in reducing food intake.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Richard L. Gelb Center for Pharmaceutical Research and Development, Wallingford, CT 06492, USA. gillmank@bms.com
authors.forename: Kevin W
authors.initials: KW
authors.lastname: Gillman
authors.forename: Mendi A
authors.initials: MA
authors.lastname: Higgins
authors.forename: Graham S
authors.initials: GS
authors.lastname: Poindexter
authors.forename: Marc
authors.initials: M
authors.lastname: Browning
authors.forename: Wendy J
authors.initials: WJ
authors.lastname: Clarke
authors.forename: Sharon
authors.initials: S
authors.lastname: Flowers
authors.forename: James E
authors.initials: JE
authors.lastname: Grace
authors.forename: John B
authors.initials: JB
authors.lastname: Hogan
authors.forename: Rachel T
authors.initials: RT
authors.lastname: McGovern
authors.forename: Lawrence G
authors.initials: LG
authors.lastname: Iben
authors.forename: Gail K
authors.initials: GK
authors.lastname: Mattson
authors.forename: Astrid
authors.initials: A
authors.lastname: Ortiz
authors.forename: Stefanie
authors.initials: S
authors.lastname: Rassnick
authors.forename: John W
authors.initials: JW
authors.lastname: Russell
authors.forename: Ildiko
authors.initials: I
authors.lastname: Antal-Zimanyi
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D004435:Eating / Q000187:drug effects*; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013997:Time Factors
chemical_list: D019440:Anti-Obesity Agents; D007093:Imidazoles; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor