Literature DB >> 19269173

7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization.

Paul V Fish1, Alan D Brown, Edel Evrard, Lee R Roberts.   

Abstract

New 7-sulfonamido-3-benzazepines 3 are disclosed as 5-HT(2C) receptor agonists. Appropriate substitution of the amino group (R(1)R(2)N-) gave compounds that were potent 5-HT(2C) agonists with minimal activation of the 5-HT(2A) and 5-HT(2B) receptors. Furthermore, representative examples had excellent in vitro ADME properties and good selectivity over ion channel activity.

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Year:  2009        PMID： 19269173     DOI： 10.1016/j.bmcl.2009.02.071

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


  3 in total

1.  Synthesis of azetidines via visible-light-mediated intermolecular [2+2] photocycloadditions.

Authors:  Marc R Becker; Emily R Wearing; Corinna S Schindler
Journal:  Nat Chem       Date:  2020-09-23       Impact factor: 24.427

2.  Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.

Authors:  Guy Rouquet; Dianna E Moore; Malcolm Spain; Daniel M Allwood; Claudio Battilocchio; David C Blakemore; Paul V Fish; Stephen Jenkinson; Alan S Jessiman; Steven V Ley; Gordon McMurray; R Ian Storer
Journal:  ACS Med Chem Lett       Date:  2015-01-20       Impact factor: 4.345

Review 3.  Synthesis of azetidines by aza Paternò-Büchi reactions.

Authors:  Alistair D Richardson; Marc R Becker; Corinna S Schindler
Journal:  Chem Sci       Date:  2020-06-12       Impact factor: 9.825
  3 in total

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