N1-Arylsulfonyl-N2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines as novel calcimimetics acting on the calcium sensing receptor

Bioorg Med Chem Lett. 2000 Sep 4;10(17):2001-4. doi: 10.1016/s0960-894x(00)00382-6.

Abstract

The synthesis and calcimimetic properties of N1-arylsulfonyl-N2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines are described. The most active compound of the series (3n, used at 10 microM) produced 97+/-11% of the maximal stimulation of [3H]IP production obtained by 10 mM Ca2+ in CHO cells expressing the calcium sensing receptor (CaSR). This calcimimetic activity was due to a specific interaction of this compound with the CaSR.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Calcium / metabolism*
  • Cricetinae
  • Diamines / chemical synthesis
  • Diamines / pharmacology*
  • Inositol Phosphates / biosynthesis
  • Receptors, Calcium-Sensing
  • Receptors, Cell Surface / drug effects*

Substances

  • Diamines
  • Inositol Phosphates
  • Receptors, Calcium-Sensing
  • Receptors, Cell Surface
  • Calcium