Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587782 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
A novel series of non-peptidic OX1R/OX2R orexin receptor antagonists was prepared by heterocyclic replacement of the dimethoxyphenyl moiety contained in the tetrahydroisoquinoline core skeleton of almorexant. Introduction of substituted imidazole moieties delivered potent dual orexin receptor antagonists with nanomolar potency for hOX1R and hOX2R suitable for further fine-tuning. The preparation of these novel orexin receptor antagonists and the outcome of preliminary structure-activity relationship studies are described in this communication.
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Authors
Thierry Sifferlen, Ralf Koberstein, Emmanuelle Cottreel, Amandine Boller, Thomas Weller, John Gatfield, Catherine Brisbare-Roch, Francois Jenck, Christoph Boss,