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Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists |
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| Authors: | Gillman Kevin W Higgins Mendi A Poindexter Graham S Browning Marc Clarke Wendy J Flowers Sharon Grace James E Hogan John B McGovern Rachel T Iben Lawrence G Mattson Gail K Ortiz Astrid Rassnick Stefanie Russell John W Antal-Zimanyi Ildiko |
| Affiliation: | Bristol-Myers Squibb Pharmaceutical Research Institute, Richard L. Gelb Center for Pharmaceutical Research and Development, Wallingford, CT 06492, USA. gillmank@bms.com |
| 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. |
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