Author/Authors :
Wu Yang، نويسنده , , Yufeng Wang، نويسنده , , Jacques Y. Roberge، نويسنده , , Zhengping Ma، نويسنده , , Yalei Liu، نويسنده , , R. Michael Lawrence، نويسنده , , David P. Rotella، نويسنده , , Ramakrishna Seethala، نويسنده , , Jean H.M Feyen، نويسنده , , John K. Dickson Jr.، نويسنده ,
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.