| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372100 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
Agonists of the 5-HT2C receptor have been shown to suppress appetite and reduce body weight in animal models as well as in humans. However, agonism of the related 5-HT2B receptor has been associated with valvular heart disease. Synthesis and biological evaluation of a series of novel and highly selective dihydroquinazolinone-derived 5-HT2C agonists with no detectable agonism of the 5-HT2B receptor is described. Among these, compounds (+)-2a and (+)-3c were identified as potent and highly selective agonists which exhibited weight loss in a rat model upon oral dosing.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Saleem Ahmad, Khehyong Ngu, Keith J. Miller, Ginger Wu, Chen-pin Hung, Sarah Malmstrom, Ge Zhang, Eva O’Tanyi, William J. Keim, Mary Jane Cullen, Kenneth W. Rohrbach, Michael Thomas, Thao Ung, Qinling Qu, Jinping Gan, Rangaraj Narayanan,