Discovery and Structure-Activity Relationships of 2-Benzylpyrrolidine- Substituted Aryloxypropanols As Calcium-Sensing Receptor Antagonists

Authors

Wu Yang, Bristol-Myers Squibb
Yufeng Wang, Bristol-Myers Squibb
Jacques Y. Roberge, Bristol-Myers Squibb
Zhengping Ma, Bristol-Myers Squibb
Yalei Liu, Bristol-Myers Squibb
R. Michael Lawrence, Bristol-Myers Squibb
David Rotella, Montclair State UniversityFollow
Ramakrishna Seethala, Bristol-Myers Squibb
Jean H.M. Feyen, Bristol-Myers Squibb
John K. Dickson, Bristol-Myers Squibb

Document Type

Article

Publication Date

2-15-2005

Journal / Book Title

Bioorganic & Medicinal Chemistry Letters

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.

DOI

10.1016/j.bmcl.2004.11.071

Montclair State University 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.
https://digitalcommons.montclair.edu/chem-biochem-facpubs/58