Title

Discovery and Structure-Activity Relationships of 2-Benzylpyrrolidine- Substituted Aryloxypropanols As Calcium-Sensing Receptor Antagonists

Document Type

Article

Publication Date

2-15-2005

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.

DOI

10.1016/j.bmcl.2004.11.071

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