Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375461 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
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.
Graphical abstractThe synthesis and structure–activity relationship study of a novel family of calcium-sensing receptor antagonists are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ashvinikumar V. Gavai, Roy J. Vaz, Amarendra B. Mikkilineni, Jacques Y. Roberge, Yalei Liu, R. Michael Lawrence, James R. Corte, Wu Yang, Mark Bednarz, John K. Dickson Jr., Zhengping Ma, Ramakrishna Seethala, Jean H.M. Feyen,