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Updated: May 13, 2026

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor
Published on: October 26, 2017
New potent calcimimetics: II. Discovery of benzothiazole trisubstituted ureas
Pierre Deprez1, Taoues Temal, Hélène Jary
1Galapagos SASU, 102 Avenue Gaston Roussel, 93230 Romainville, France. pierre.deprez@glpg.com
Abstract:
Following the identification of trisubstituted ureas as a promising new chemical series of allosteric modulators of the calcium sensing receptor (CaSR), we further explored the SAR around the urea substitution, leading to the discovery of benzothiazole urea compound 13. This compound is a potent calcimimetic with an EC50=20 nM (luciferase assay). Evaluated in an in vivo model of chronic renal failure (short term and long term in 5/6 nephrectomized rats), benzothiazole urea 13 significantly decreased PTH levels after oral administration while keeping calcemia within the normal range.
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