1. Academic Validation
  2. The discovery of novel calcium sensing receptor negative allosteric modulators

The discovery of novel calcium sensing receptor negative allosteric modulators

  • Bioorg Med Chem Lett. 2009 Jun 15;19(12):3328-32. doi: 10.1016/j.bmcl.2009.04.044.
Gayatri Balan 1 Jonathan Bauman Samit Bhattacharya Mayda Castrodad David R Healy Michael Herr Paul Humphries Sandra Jennings Amit S Kalgutkar Brendon Kapinos Vishal Khot Kimberly Lazarra Mei Li Yan Li Constantin Neagu Robert Oliver David W Piotrowski David Price Hong Qi Holly A Simmons James Southers Liuqing Wei Yan Zhang Vishwas M Paralkar
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Groton/New London Laboratories, Pfizer Inc., Eastern Point Road, Groton, CT 06340, USA.
Abstract

The design and profile of a series of zwitterionic calcium sensing receptor negative allosteric modulators is described. Evaluation of key analogues using a rat model demonstrate a robust response, significantly improved potency over ronacaleret and have the potential as an oral, anabolic treatment for osteoporosis.

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