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
  • 1. Pfizer Global Research and Development, Groton/New London Laboratories, Pfizer Inc., Eastern Point Road, Groton, CT 06340, USA.
PMID: 19442519 DOI: 10.1016/j.bmcl.2009.04.044
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.