Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
5 years ago

Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration

Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration
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).

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X1730896X

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