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

Authors :
Yang, Wu
Wang, Yufeng
Roberge, Jacques Y.
Ma, Zhengping
Liu, Yalei
Michael Lawrence, R.
Rotella, David P.
Seethala, Ramakrishna
Feyen, Jean H.M.
Dickson, John K.
Source :
Bioorganic & Medicinal Chemistry Letters. Feb2005, Vol. 15 Issue 4, p1225-1228. 4p.
Publication Year :
2005

Abstract

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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
15
Issue :
4
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
16203987
Full Text :
https://doi.org/10.1016/j.bmcl.2004.11.071