New potent calcimimetics: I. Discovery of a series of novel trisubstituted ureas.
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Temal T, Jary H, Auberval M, Lively S, Guedin D, Vevert JP, Deprez P
New potent calcimimetics: I. Discovery of a series of novel trisubstituted ureas.
Bioorg Med Chem Lett. 2013 Apr 15;23(8):2451-4. doi: 10.1016/j.bmcl.2013.01.078. Epub 2013 Jan 29.
- PubMed ID
- 23465611 [ View in PubMed]
- Abstract
Starting from Fendiline and R-568, we identified a novel series of urea compounds as positive allosteric modulators of the calcium sensing receptor (CaSR), as part of a program to identify novel therapeutics for secondary hyperparathyroidism. Initially identified disubstituted ureas were converted to trisubstituted urea lead 20e, which was further modified to increase in vivo potency. Replacing a carbomethoxy substituent by various bioisosteres led to compound 46 which exhibited potent in vitro and in vivo activity after oral administration.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Cinacalcet Extracellular calcium-sensing receptor EC 50 (nM) 80 N/A N/A Details