Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists |
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| 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 |
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| Affiliation: | Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5400, Princeton, NJ 08543-5400, USA. wu.yang@bms.com |
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| 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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