Discovery of novel dihydrobenzofuran cyclopropane carboxylic acid based calcium sensing receptor antagonists for the treatment of osteoporosis.
2016
Abstract In a search for novel small molecule
calcium-sensing receptor(CaSR) antagonists as oral bone
anabolicagents, we discovered dihydrobenzofuran
cyclopropanecarboxylic acid derivatives, such as 12f (IC 50 = 27.6 nM), are highly potent
calcium-sensing receptorantagonists. Studies in rats established that compound 12f stimulates
parathyroid hormone(PTH) release in a fast-acting, pulsatile manner.
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