New aminopropandiol derivatives as orally available and short-acting calcium-sensing receptor antagonists

  • Bioorg Med Chem Lett. 2010 Jun 15;20(12):3809-13. doi: 10.1016/j.bmcl.2010.04.035.
Yuko Shinagawa  1 ,  Teruhiko Inoue ,  Kazuyuki Hirata ,  Takeo Katsushima ,  Takashi Nakagawa ,  Yushi Matsuo ,  Masanori Shindo ,  Hiromasa Hashimoto
Affiliations
  • 1. Central Pharmaceutical Research Institute, Japan Tobacco Inc., Takatsuki, Osaka, Japan. [email protected]
PMID: 20472433 DOI: 10.1016/j.bmcl.2010.04.035
Abstract

Synthesis and structure-activity relationship studies on a new aminopropandiol class of derivatives as calcium-sensing receptor antagonists are described. Modification of the phenolic moiety of a calcilytic compound NPS 2143 led to the identification of an orally available compound (R,R)-31 which demonstrated a rapid and transient stimulation of PTH release in rats.