Discovery and Characterization of Novel, Potent, Non-Peptide Parathyroid Hormone-1 Receptor Antagonists

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• 作者：Iain M. McDonald ; 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
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：October 4, 2007
• 年：2007
• 卷：50
• 期：20
• 页码：4789 - 4792
• 全文大小：64K
• 年卷期：v.50,no.20(October 4, 2007)
• ISSN：1520-4804

文摘

A 1,3,4-benzotriazepine was identified as a suitable lead inour effort toward obtaining a non-peptide parathyroid hormone-1receptor (PTH₁R) antagonist. A process of optimization affordedderivatives displaying nanomolar PTH₁R affinity, a representativeexample of which behaved as a PTH₁R antagonist in cell-based cyclicadenosine monophosphate (cAMP) assays, with selectivity over PTH₂receptors.