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

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

  • Bioorg Med Chem Lett. 2005 Dec 15;15(24):5478-82. doi: 10.1016/j.bmcl.2005.08.095.
Ashvinikumar V Gavai 1,  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
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. ashvinikumar.gavai@bms.com
PMID: 16216508 DOI: 10.1016/j.bmcl.2005.08.095
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.

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