Article ID Journal Published Year Pages File Type
1375461 Bioorganic & Medicinal Chemistry Letters 2005 5 Pages PDF
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
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