Title of article
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
5478
To page
5482
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.
Keywords
Osteoporosis , Calcium-sensing receptor antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796212
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