Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis |
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Authors: | Leila Malik Nicholas M Kelly Jian-Nong Ma Erika A Currier Ethan S Burstein Roger Olsson |
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Institution: | 1. ACADIA Pharmaceuticals AB, Medeon Science Park, S-205 12 Malmö, Sweden;2. ACADIA Pharmaceuticals Inc., 3911 Sorrento Valley Blvd., San Diego, CA 92121, USA |
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Abstract: | A class of small molecules displaying comparable activities with peptide ligands BAM22 and corticostatin-14 at both the human and rhesus monkey MrgX1 and MrgX2 receptors, respectively, was discovered. A comparative study to compare solid-phase and solution-phase chemistries for the efficient synthesis of the active class, tetracyclic benzimidazoles, was undertaken. The solid-phase chemistry was found to be superior both for the synthesis of analogs and for the synthesis of gram quantities. |
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