3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1557-60. doi: 10.1016/j.bmcl.2005.01.078.

Abstract

Structure-activity relationship studies, focused on identification of the active pharmacophore fragments in a single high-throughput screening calcilytic hit, resulted in the discovery of potent calcium receptor antagonists, substituted 3H-quinazolin-4-ones.

MeSH terms

  • Animals
  • Male
  • Models, Chemical
  • Molecular Structure
  • Osteoporosis / drug therapy
  • Parathyroid Hormone / blood
  • Quinazolines / chemistry*
  • Quinazolines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Calcium-Sensing / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • NPS53574
  • Parathyroid Hormone
  • Quinazolines
  • Receptors, Calcium-Sensing