Bioorganic & Medicinal Chemistry Letters 2010-09-15

The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core.

Paul E Harrington, David J St Jean, Jeffrey Clarine, Thomas S Coulter, Michael Croghan, Adam Davenport, James Davis, Chiara Ghiron, Jonathan Hutchinson, Michael G Kelly, Fred Lott, Jenny Ying-Lin Lu, David Martin, Sean Morony, Steve F Poon, Elena Portero-Larragueta, Jeff D Reagan, Kelly A Regal, Andrew Tasker, Minghan Wang, Yuhua Yang, Guomin Yao, Qingping Zeng, Charles Henley, Christopher Fotsch

Index: Bioorg. Med. Chem. Lett. 20(18) , 5544-7, (2010)

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Abstract

The discovery of a series of novel and orally efficacious type II calcimimetics, developed from the lead compound 1, is described herein. Compound 22 suppressed plasma PTH levels relative to vehicle when dosed orally in a rat pharmacodynamic model.Copyright (c) 2010 Elsevier Ltd. All rights reserved.