|
|||||
|
|
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents |
|
| 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 Mary Ann Pelleymounter Jeffrey A. Robl |
| Affiliation: | Research & Development, Bristol-Myers Squibb Co, PO Box 4000, Princeton, NJ 08543, United States |
| 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. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |