Discovery and Structure-Activity Relationships of 2-Benzylpyrrolidine- Substituted Aryloxypropanols As Calcium-Sensing Receptor Antagonists
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.
MSU Digital Commons Citation
Yang, Wu; Wang, Yufeng; Roberge, Jacques Y.; Ma, Zhengping; Liu, Yalei; Lawrence, R. Michael; Rotella, David; Seethala, Ramakrishna; Feyen, Jean H.M.; and Dickson, John K., "Discovery and Structure-Activity Relationships of 2-Benzylpyrrolidine- Substituted Aryloxypropanols As Calcium-Sensing Receptor Antagonists" (2005). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 58.