Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis.
Basic Information
ID: ALA3826945
Journal: Bioorg Med Chem Lett
Title: Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis.
Authors: Liang GB, Zhou C, Huo X, Wang H, Yang X, Huang S, Wang H, Wilkinson H, Luo L, Tang W, Sutton D, Li H, Zaller D, Meinke PT.
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.
CiteXplore: 27397499
DOI: 10.1016/j.bmcl.2016.06.073
Patent ID: ┄