Literature DB >> 23177783

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

John M Fevig1, Jianxin Feng, Karen A Rossi, Keith J Miller, Ginger Wu, Chen-Pin Hung, Thao Ung, Sarah E Malmstrom, Ge Zhang, William J Keim, Mary Jane Cullen, Kenneth W Rohrbach, Qinling Qu, Jinping Gan, Mary Ann Pelleymounter, Jeffrey A Robl.   

Abstract

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.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23177783     DOI: 10.1016/j.bmcl.2012.10.091

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  An efficient route to N-alkylated 3,4-dihydroisoquinolinones with substituents at the 3-position.

Authors:  Aoi Tazawa; Junki Ando; Kohei Ishizawa; Isao Azumaya; Hidemasa Hikawa; Minoru Tanaka
Journal:  RSC Adv       Date:  2018-02-07       Impact factor: 3.361

  1 in total

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