| Literature DB >> 20022752 |
Saleem Ahmad1, 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.
Abstract
Agonists of the 5-HT(2C) 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-HT(2B) receptor has been associated with valvular heart disease. Synthesis and biological evaluation of a series of novel and highly selective dihydroquinazolinone-derived 5-HT(2C) agonists with no detectable agonism of the 5-HT(2B) 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. Copyright (c) 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20022752 DOI： 10.1016/j.bmcl.2009.12.014
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823