Literature DB >> 24630562

Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.

Scott D Kuduk1, Jason W Skudlarek2, Christina N Di Marco2, Joseph G Bruno3, Mark A Pausch3, Julie A O'Brien3, Tamara D Cabalu4, Joanne Stevens5, Joseph Brunner5, Pamela L Tannenbaum5, Anthony L Gotter6, Christopher J Winrow6, John J Renger6, Paul J Coleman2.   

Abstract

Analogs of the dual orexin receptor antagonist filorexant were prepared. Replacement of the ether linkage proved highly sensitive toward modification with an acetylene linkage providing compounds with the best in vitro and in vivo potency profiles.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antagonist; Insomnia; Orexin

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Substances:

Year:  2014        PMID: 24630562     DOI: 10.1016/j.bmcl.2014.02.026

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


  1 in total

1.  Antitrypanosomatid Pharmacomodulation at Position 3 of the 8-Nitroquinolin-2(1H)-one Scaffold Using Palladium-Catalysed Cross-Coupling Reactions.

Authors:  Julien Pedron; Clotilde Boudot; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Lucie Paloque; Maryam Rastegari; Mansour Abdoulaye; Hussein El-Kashef; Colin Bonduelle; Geneviève Pratviel; Susan Wyllie; Alan H Fairlamb; Bertrand Courtioux; Pierre Verhaeghe; Alexis Valentin
Journal:  ChemMedChem       Date:  2018-09-17       Impact factor: 3.466

  1 in total

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