Author/Authors :
Ashvinikumar V. Gavai، نويسنده , , Roy J. Vaz، نويسنده , , Amarendra B. Mikkilineni، نويسنده , , Jacques Y. Roberge، نويسنده , , Yalei Liu، نويسنده , , R. Michael Lawrence، نويسنده , , James R. Corte، نويسنده , , Wu Yang، نويسنده , , Mark Bednarz، نويسنده , , John K. Dickson Jr.، نويسنده , , Zhengping Ma، نويسنده , , Ramakrishna Seethala، نويسنده , , Jean H.M Feyen، نويسنده ,
Abstract :
A 3D quantitative structure–activity relationship study for inhibition of calcium-sensing receptor in the aryloxypropanolamine series predicted that these molecules adopt a U-shaped conformation with pi-stacking between the two aromatic rings. This hypothesis led to the discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines capable of antagonizing the calcium-sensing receptor with potency comparable to that of NPS-2143.
