4.5 Article

New aminopropandiol derivatives as orally available and short-acting calcium-sensing receptor antagonists

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 12, 页码 3809-3813

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.035

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Calcium-sensing receptor; Antagonist; CaSR antagonist; PTH; Osteoporosis; Calcilytics

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Synthesis and structure-activity relationship studies on a new aminopropandiol class of derivatives as calcium-sensing receptor antagonists are described. Modification of the phenolic moiety of a calcilytic compound NPS 2143 led to the identification of an orally available compound (R,R)-31 which demonstrated a rapid and transient stimulation of PTH release in rats. (C) 2010 Elsevier Ltd. All rights reserved.

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