Literature DB >> 29937060

Design and synthesis of bridged piperidine and piperazine isosteres.

Gaëtan Maertens1, Oscar M Saavedra1, Vito Vece1, Miguel A Vilchis Reyes1, Sofiane Hocine1, Esat Öney1, Bertrand Goument2, Olivier Mirguet2, Arnaud Le Tiran2, Philippe Gloanec2, Stephen Hanessian3.   

Abstract

We have developed versatile methods toward the synthesis of a variety of piperidine/piperazine bridged isosteres of pridopidine. The compounds were assessed against the D2 receptor in agonist and antagonist modes and against the D4 receptor in agonist mode. hERG Binding and the ADME profiles were studied.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  C-arylation; Constrained amines; Dopaminergic activity; Oxabicyclic piperazines; Oxabicyclic piperidines

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Year:  2018        PMID: 29937060     DOI: 10.1016/j.bmcl.2018.06.038

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


  1 in total

1.  Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.

Authors:  Joseph Carpenter; Gang Wu; Ying Wang; Erica M Cook; Tao Wang; Doree Sitkoff; Karen A Rossi; Kathy Mosure; Xiaoliang Zhuo; Gary G Cao; Milinda Ziegler; Anthony V Azzara; Jack Krupinski; Matthew G Soars; Bruce Alan Ellsworth; Dean A Wacker
Journal:  ACS Med Chem Lett       Date:  2021-08-05       Impact factor: 4.632

  1 in total

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