Literature DB >> 20015649

Biaryl piperidines as potent and selective delta opioid receptor ligands.

Spiros Liras1, Stanton F McHardy, Martin P Allen, Barb E Segelstein, Steven D Heck, Dianne K Bryce, Anne W Schmidt, Michelle Vanase-Frawley, Ernesto Callegari, Stafford McLean.   

Abstract

The design and synthesis of novel opiates are reported. Based on the message-address principle a novel class of 4,4- and 3,3-biaryl piperidines was designed and synthesized. Biological evaluation confirmed that these compounds exhibit high affinity and selectivity for the delta opioid receptor. Key structure-activity relationships that influence affinity, selectivity, functional activity and clearance are reported. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID: 20015649     DOI: 10.1016/j.bmcl.2009.11.113

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


  3 in total

1.  Synthesis of bis-spirocyclic derivatives of 3-azabicyclo[3.1.0]hexane via cyclopropene cycloadditions to the stable azomethine ylide derived from Ruhemann's purple.

Authors:  Alexander S Filatov; Olesya V Khoroshilova; Anna G Larina; Vitali M Boitsov; Alexander V Stepakov
Journal:  Beilstein J Org Chem       Date:  2022-06-29       Impact factor: 2.544

2.  Synthesis of CHF2-substituted 3-azabicyclo[3.1.0]hexanes by photochemical decomposition of CHF2-pyrazolines.

Authors:  Yang Zheng; Xinling Yu; Songyang Lv; Pavel K Mykhailiuk; Qiang Ma; Li Hai; Yong Wu
Journal:  RSC Adv       Date:  2018-01-29       Impact factor: 4.036

3.  Tandem dinucleophilic cyclization of cyclohexane-1,3-diones with pyridinium salts.

Authors:  Mostafa Kiamehr; Firouz Matloubi Moghaddam; Satenik Mkrtchyan; Volodymyr Semeniuchenko; Linda Supe; Alexander Villinger; Peter Langer; Viktor O Iaroshenko
Journal:  Beilstein J Org Chem       Date:  2013-06-10       Impact factor: 2.883

  3 in total

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