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 language | English |
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Pages (from-to) | 1225-1228 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 15 |
Issue number | 4 |
DOIs | |
State | Published - 15 Feb 2005 |
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Keywords
- Calcium-sensing receptor antagonist
- Osteoporosis
Cite this
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Discovery and structure-activity relationships of 2-benzylpyrrolidine- substituted aryloxypropanols as calcium-sensing receptor antagonists. / Yang, Wu; Wang, Yufeng; Roberge, Jacques Y.; Ma, Zhengping; Liu, Yalei; Lawrence, R. Michael; Rotella, David; Seethala, Ramakrishna; Feyen, Jean H.M.; Dickson, John K.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 15, No. 4, 15.02.2005, p. 1225-1228.Research output: Contribution to journal › Article
TY - JOUR
T1 - Discovery and structure-activity relationships of 2-benzylpyrrolidine- substituted aryloxypropanols as calcium-sensing receptor antagonists
AU - Yang, Wu
AU - Wang, Yufeng
AU - Roberge, Jacques Y.
AU - Ma, Zhengping
AU - Liu, Yalei
AU - Lawrence, R. Michael
AU - Rotella, David
AU - Seethala, Ramakrishna
AU - Feyen, Jean H.M.
AU - Dickson, John K.
PY - 2005/2/15
Y1 - 2005/2/15
N2 - 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.
AB - 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.
KW - Calcium-sensing receptor antagonist
KW - Osteoporosis
UR - http://www.scopus.com/inward/record.url?scp=20144387408&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2004.11.071
DO - 10.1016/j.bmcl.2004.11.071
M3 - Article
C2 - 15686947
AN - SCOPUS:20144387408
VL - 15
SP - 1225
EP - 1228
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 4
ER -