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

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

  • Bioorg Med Chem Lett. 2005 Feb 15;15(4):1225-8. doi: 10.1016/j.bmcl.2004.11.071.
Wu Yang 1,  Yufeng Wang,  Jacques Y Roberge,  Zhengping Ma,  Yalei Liu,  R Michael Lawrence,  David P Rotella,  Ramakrishna Seethala,  Jean H M Feyen,  John K Dickson Jr
Affiliations

Affiliation

  • 1 Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5400, Princeton, NJ 08543-5400, USA. wu.yang@bms.com
PMID: 15686947 DOI: 10.1016/j.bmcl.2004.11.071
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.

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