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Bioorg Med Chem Lett. 2005 Dec 15;15(24):5478-82. Epub 2005 Oct 10.

Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.

Author information

1
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. ashvinikumar.gavai@bms.com

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.

PMID:
16216508
DOI:
10.1016/j.bmcl.2005.08.095
[Indexed for MEDLINE]

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