New potent calcimimetics: I. Discovery of a series of novel trisubstituted ureas

T Temal, H Jary, M Auberval, S Lively, D Guédin…

文献索引：Temal, Taoues; Jary, Helene; Auberval, Marielle; Lively, Sarah; Guedin, Denis; Vevert, Jean-Paul; Deprez, Pierre Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 8 p. 2451 - 2454

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被引用次数: 4

摘要

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 ...