|
|||||
|
|
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 |
| Institution: | 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！ | |