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. 2007 Oct 4;50(20):4789-92.
doi: 10.1021/jm0707626. Epub 2007 Sep 12.

Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists

Iain M McDonald  1 , Carol Austin, Ildiko M Buck, David J Dunstone, John Gaffen, Eric Griffin, Elaine A Harper, Robert A D Hull, S Barret Kalindjian, Ian D Linney, Caroline M R Low, Dipa Patel, Michael J Pether, Michelle Raynor, Sonia P Roberts, Mark E Shaxted, John Spencer, Katherine I M Steel, David A Sykes, Paul T Wright, Wei Xun
Affiliations

Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists

Iain M McDonald et al. J Med Chem. .

Abstract

A 1,3,4-benzotriazepine was identified as a suitable lead in our effort toward obtaining a non-peptide parathyroid hormone-1 receptor (PTH1R) antagonist. A process of optimization afforded derivatives displaying nanomolar PTH1R affinity, a representative example of which behaved as a PTH1R antagonist in cell-based cyclic adenosine monophosphate (cAMP) assays, with selectivity over PTH2 receptors.

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