Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists

Autor:	Keith J. Miller, Kenneth W. Rohrbach, Jianxin Feng, Mary Ann Pelleymounter, Sarah E. Malmstrom, Jinping Gan, Ge Zhang, Ginger Wu, Thao Ung, Chen-Pin Hung, William J. Keim, Karen A. Rossi, Jeffrey A. Robl, Qinling Qu, John M. Fevig, Mary Jane Cullen
Rok vydání:	2013
Předmět:	Male Food intake Stereochemistry Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry Rats sprague dawley Rats Sprague-Dawley Structure-Activity Relationship Receptor Serotonin 5-HT2B Drug Discovery Receptor Serotonin 5-HT2C Animals Humans Structure–activity relationship Pyrroles Receptor Serotonin 5-HT2A Receptor Molecular Biology 5-HT receptor Chemistry Organic Chemistry Isoquinolines Rats 5-HT2C receptor Molecular Medicine Serotonin Selectivity Heterocyclic Compounds 3-Ring Serotonin 5-HT2 Receptor Agonists Half-Life
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 23:330-335
ISSN:	0960-894X
Popis:	A series of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones is described, several examples of which exhibit potent 5-HT(2C) agonism with excellent selectivity over the closely related 5-HT(2A) and 5-HT(2B) receptors. Compounds such as 38 and 44 were shown to be effective in reducing food intake in an acute rat feeding model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2079c57086a886d54141aa8d75f1c8e7 https://doi.org/10.1016/j.bmcl.2012.10.091 Zobrazit plný text záznamu Full Text from ScienceDirect