Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration.
Basic Information
ID: ALA4043225
Journal: Bioorg Med Chem Lett
Title: Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration.
Authors: Sparks SM, Spearing PK, Diaz CJ, Cowan DJ, Jayawickreme C, Chen G, Rimele TJ, Generaux C, Harston LT, Roller SG.
Abstract: Modulation of gastrointestinal nutrient sensing pathways provides a promising a new approach for the treatment of metabolic diseases including diabetes and obesity. The calcium-sensing receptor has been identified as a key receptor involved in mineral and amino acid nutrient sensing and thus is an attractive target for modulation in the intestine. Herein we describe the optimization of gastrointestinally restricted calcium-sensing receptor agonists starting from a 3-aminopyrrolidine-containing template leading to the identification of GI-restricted agonist 19 (GSK3004774).
CiteXplore: 28916340
DOI: 10.1016/j.bmcl.2017.09.008
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