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

…, Y Liu, RM Lawrence, DP Rotella, R Seethala…

Index: Yang, Wu; Wang, Yufeng; Roberge, Jacques Y.; Ma, Zhengping; Liu, Yalei; Lawrence, R. Michael; Rotella, David P.; Seethala, Ramakrishna; Feyen, Jean H. M.; Dickson Jr., John K. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 4 p. 1225 - 1228

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Citation Number: 35

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.