Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis. Academic Article uri icon

Overview

abstract

  • In a search for novel small molecule calcium-sensing receptor (CaSR) antagonists as oral bone anabolic agents, we discovered dihydrobenzofuran cyclopropane carboxylic acid derivatives, such as 12f (IC50=27.6nM), are highly potent calcium-sensing receptor antagonists. Studies in rats established that compound 12f stimulates parathyroid hormone (PTH) release in a fast-acting, pulsatile manner.

publication date

  • June 29, 2016

Research

keywords

  • Benzofurans
  • Cyclopropanes
  • Osteoporosis
  • Receptors, Calcium-Sensing

Identity

Scopus Document Identifier

  • 84979517641

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2016.06.073

PubMed ID

  • 27397499

Additional Document Info

volume

  • 26

issue

  • 16