Discovery and structure-activity relationships of 2-benzylpyrrolidine- substituted aryloxypropanols as calcium-sensing receptor antagonists

Wu Yang, Yufeng Wang, Jacques Y. Roberge, Zhengping Ma, Yalei Liu, R. Michael Lawrence, David Rotella, Ramakrishna Seethala, Jean H.M. Feyen, John K. Dickson

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Abstract

A structure-activity relationship study of the amine portion of the calcilytic compound NPS-2143 resulted in the discovery of substituted 2-benzylpyrrolidines as replacements for the 1,1-dimethyl-2-naphthalen-2-yl- ethylamine. When compared to NPS-2143, a newly discovered compound, 3h, exhibited similar potency as a calcium-sensing receptor (CaR) antagonist and a superior human ether-a-go-go related gene (hERG) profile.

Original languageEnglish
Pages (from-to)1225-1228
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number4
DOIs
StatePublished - 15 Feb 2005

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Keywords

  • Calcium-sensing receptor antagonist
  • Osteoporosis

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